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Carbon Dots as a Fluorescent Nanosystem for Crossing the Blood–Brain Barrier with Plausible Application in Neurological Diseases
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A Bionic “Trojan Horse”-like Nanovesicle Delivery System Hybridized with BCG Cytoplasmic Membrane and Melanoma Cell Membrane for Cancer Immunotherapy
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Microfluidic Optimization of PEI-Lipid Hybrid Nanoparticles for Efficient DNA Delivery and Transgene Expression
Journal Description
Pharmaceutics
Pharmaceutics
is a peer-reviewed, open access journal on the science and technology of pharmaceutics and biopharmaceutics, and is published monthly online by MDPI. The Spanish Society of Pharmaceutics and Pharmaceutical Technology (SEFIG), Pharmaceutical Solid State Research Cluster (PSSRC), Academy of Pharmaceutical Sciences (APS) and Korean Society of Pharmaceutical Sciences and Technology (KSPST) are affiliated with Pharmaceutics and their members receive a discount on the article processing charges.
- Open Access— free for readers, with article processing charges (APC) paid by authors or their institutions.
- High Visibility: indexed within Scopus, SCIE (Web of Science), PubMed, PMC, Embase, CAPlus / SciFinder, and other databases.
- Journal Rank: JCR - Q1 (Pharmacology and Pharmacy) / CiteScore - Q1 (Pharmaceutical Science)
- Rapid Publication: manuscripts are peer-reviewed and a first decision is provided to authors approximately 14.9 days after submission; acceptance to publication is undertaken in 3.3 days (median values for papers published in this journal in the first half of 2025).
- Recognition of Reviewers: reviewers who provide timely, thorough peer-review reports receive vouchers entitling them to a discount on the APC of their next publication in any MDPI journal, in appreciation of the work done.
- Companion journals for Pharmaceutics include: Future Pharmacology, Journal of Pharmaceutical and BioTech Industry and Medicines.
- Journal Clusters-Pharmaceutical Science: Scientia Pharmaceutica, Pharmaceuticals, Pharmaceutics, Pharmacy, Future Pharmacology, Pharmacoepidemiology, Drugs and Drug Candidates and Journal of Pharmaceutical and BioTech Industry.
Impact Factor:
5.5 (2024);
5-Year Impact Factor:
5.8 (2024)
Latest Articles
Preclinical Trials of Cancer Stem Cells Targeted by Metal-Based Coordination Complexes: A Systematic Review
Pharmaceutics 2025, 17(7), 931; https://doi.org/10.3390/pharmaceutics17070931 - 18 Jul 2025
Abstract
Background/Objective: Cancer stem cells (CSCs) are a self-renewing subpopulation within tumors that contribute to heterogeneity and resistance to conventional cancer therapies, including chemotherapy and radiotherapy. Despite growing interest in CSCs as therapeutic targets, effective compounds against these cells remain limited. This systematic
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Background/Objective: Cancer stem cells (CSCs) are a self-renewing subpopulation within tumors that contribute to heterogeneity and resistance to conventional cancer therapies, including chemotherapy and radiotherapy. Despite growing interest in CSCs as therapeutic targets, effective compounds against these cells remain limited. This systematic review aims to assess the potential of metal-based coordination complexes as anti-CSC agents in preclinical models. Methods: A systematic literature search was conducted following the Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA) guidelines. Twenty-seven original in vitro studies were included, all evaluating the cytotoxic effects of metal-based compounds on cancer cell lines enriched with CSC subpopulations. To ensure methodological rigor, all articles underwent a critical appraisal by independent reviewers who resolved discrepancies through consensus, and only studies meeting predefined quality criteria were included. Results: Several metal complexes, particularly copper-based compounds, demonstrated significant cytotoxicity toward CSCs, mainly through the induction of apoptosis. Breast cancer was the most frequently studied tumor type. Many studies reported modulation of CSC-related markers, including EPCAM, CD44, CD133, CD24, SOX2, KLF4, Oct4, NOTCH1, ALDH1, CXCR4, and HES1, suggesting effects on CSC maintenance pathways. Most studies were conducted in the United Kingdom and relied on in vitro models. Conclusions: Metal coordination complexes, especially those containing copper, show promise as therapeutic agents targeting CSCs. However, further in vivo studies and mechanistic investigations are essential to advance their translational potential.
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(This article belongs to the Topic Recent Advances in Anticancer Strategies, 2nd Edition)
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Open AccessReview
MicroRNA-Based Delivery Systems for Chronic Neuropathic Pain Treatment in Dorsal Root Ganglion
by
Stefan Jackson, Maria Rosa Gigliobianco, Cristina Casadidio, Piera Di Martino and Roberta Censi
Pharmaceutics 2025, 17(7), 930; https://doi.org/10.3390/pharmaceutics17070930 - 18 Jul 2025
Abstract
Neuropathic pain is a significant global clinical issue that poses substantial challenges to both public health and the economy due to its complex underlying mechanisms. It has emerged as a serious health concern worldwide. Recent studies involving dorsal root ganglion (DRG) stimulation have
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Neuropathic pain is a significant global clinical issue that poses substantial challenges to both public health and the economy due to its complex underlying mechanisms. It has emerged as a serious health concern worldwide. Recent studies involving dorsal root ganglion (DRG) stimulation have provided strong evidence supporting its effectiveness in alleviating chronic pain and its potential for sustaining long-term pain relief. In addition to that, there has been ongoing research with clinical evidence relating to the role of small non-coding ribonucleic acids known as microRNAs in regulating gene expressions affecting pain signals. The signal pathway involves alterations in neuronal excitation, synaptic transmission, dysregulated signaling, and subsequent pro-inflammatory response activation and pain development. When microRNAs are dysregulated in the dorsal root ganglia neurons, they polarize macrophages from anti-inflammatory M2 to inflammatory M1 macrophages causing pain signal generation. By reversing this polarization, a therapeutic activity can be induced. However, the direct delivery of these nucleotides has been challenging due to limitations such as rapid clearance, degradation, and reduction in half-life. Therefore, safe and efficient carrier vehicles are fundamental for microRNA delivery. Here, we present a comprehensive analysis of miRNA-based nano-systems for chronic neuropathic pain, focusing on their impact in dorsal root ganglia. This review provides a critical evaluation of various delivery platforms, including viral, polymeric, lipid-based, and inorganic nanocarriers, emphasizing their therapeutic potential as well as their limitations in the treatment of chronic neuropathic pain. Innovative strategies such as hybrid nanocarriers and stimulus-responsive systems are also proposed to enhance the prospects for clinical translation. Serving as a roadmap for future research, this review aims to guide the development and optimization of miRNA-based therapies for effective and sustained neuropathic pain management.
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(This article belongs to the Section Nanomedicine and Nanotechnology)
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Open AccessArticle
Development of a Rapid Method for Residence Time Distribution Measurement in Twin-Screw Wet Granulation Based on Image Processing with Lab Color Space
by
Jie Zhao, Geng Tian, Ying Tian and Haibin Qu
Pharmaceutics 2025, 17(7), 929; https://doi.org/10.3390/pharmaceutics17070929 - 18 Jul 2025
Abstract
Background/Objectives: In the twin-screw wet granulation (TSWG) process, accurate measurement of residence time distribution (RTD) is critical, as it characterizes material transport kinetics and mixing behavior. It plays a critical role in evaluating the homogeneity and stability of the granulation process and
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Background/Objectives: In the twin-screw wet granulation (TSWG) process, accurate measurement of residence time distribution (RTD) is critical, as it characterizes material transport kinetics and mixing behavior. It plays a critical role in evaluating the homogeneity and stability of the granulation process and optimizing process parameters. It is necessary to overcome the limitations arising from the complex and time-consuming procedures of conventional RTD determination methods. Methods: This study proposes a new RTD detection method based on image processing. It uses black dye as a tracer to obtain RTD curve data, and the effects of process parameters such as tracer dosage, screw speed, and feeding rate on the RTD were investigated. Results: The results show that the established method can accurately determine RTD and that the tracer dosage has no significant effect on the detection results. Further analysis revealed that the screw speed is negatively correlated with the mean residence time (MRT). As the speed increases, not only does the MRT shorten, but its distribution also decreases. Similarly, an increase in the feeding rate also leads to a decrease in the MRT and distribution, but it is worth noting that lower feeding rates are beneficial for achieving a state close to mixed flow, while excessively high feeding rates are not conducive to sufficient mixing of materials in the extruder. Conclusions: The RTD detection method provides a reliable parameter basis and theoretical guidance for the in-depth study of the TSWG process and the development of quality control strategies.
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(This article belongs to the Section Pharmaceutical Technology, Manufacturing and Devices)
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Comprehensive Investigation of Polymorphic Stability and Phase Transformation Kinetics in Tegoprazan
by
Joo Ho Lee, Ki Hyun Kim, Se Ah Ryu, Jason Kim, Kiwon Jung, Ki Sung Kang and Tokutaro Yamaguchi
Pharmaceutics 2025, 17(7), 928; https://doi.org/10.3390/pharmaceutics17070928 - 18 Jul 2025
Abstract
Background/Objectives: Tegoprazan (TPZ) is a potassium-competitive acid blocker (P-CAB) used to treat conditions such as gastroesophageal reflux disease, peptic ulcer, and Helicobacter pylori infection. It exists in three solid forms: amorphous, Polymorph A, and Polymorph B. This study investigates the molecular basis of
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Background/Objectives: Tegoprazan (TPZ) is a potassium-competitive acid blocker (P-CAB) used to treat conditions such as gastroesophageal reflux disease, peptic ulcer, and Helicobacter pylori infection. It exists in three solid forms: amorphous, Polymorph A, and Polymorph B. This study investigates the molecular basis of polymorph selection, focusing on conformational bias and solvent-mediated phase transformations (SMPTs). Methods: The conformational energy landscapes of two TPZ tautomers were constructed using relaxed torsion scans with the OPLS4 force field and validated by nuclear Overhauser effect (NOE)-based nuclear magnetic resonance (NMR). Hydrogen-bonded dimers were analyzed using DFT-D. Powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), solubility, and slurry tests were conducted using methanol, acetone, and water. Kinetic profiles were modeled with the Kolmogorov–Johnson–Mehl–Avrami (KJMA) equation. Results: Polymorph A was thermodynamically stable across all analyses. Both amorphous TPZ and Polymorph B converted to A in a solvent-dependent manner. Methanol induced direct A formation, while acetone showed a B → A transition. Crystallization was guided by solution conformers and hydrogen bonding. Conclusions: TPZ polymorph selection is governed by solution-phase conformational preferences, tautomerism, and solvent-mediated hydrogen bonding. DFT-D and NMR analyses showed that protic solvents favor the direct crystallization of stable Polymorph A, while aprotic solvents promote the transient formation of metastable Polymorph B. Elevated temperatures and humidity accelerate polymorphic transitions. This crystal structure prediction (CSP)-independent strategy offers a practical framework for rational polymorph control and the mitigation of disappearing polymorph risks in tautomeric drugs.
Full article
(This article belongs to the Special Issue Drug Polymorphism and Dosage Form Design, 2nd Edition)
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Open AccessReview
From Structure to Function: The Promise of PAMAM Dendrimers in Biomedical Applications
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Said Alamos-Musre, Daniel Beltrán-Chacana, Juan Moyano, Valeria Márquez-Miranda, Yorley Duarte, Sebastián Miranda-Rojas, Yusser Olguín, Juan A. Fuentes, Danilo González-Nilo and María Carolina Otero
Pharmaceutics 2025, 17(7), 927; https://doi.org/10.3390/pharmaceutics17070927 - 18 Jul 2025
Abstract
PAMAM dendrimers are distinguished by their capacity for functionalization, which enhances the properties of the compounds they transport, rendering them highly versatile nanoparticles with extensive applications in the biomedical domain, including drug, vaccine, and gene delivery. These dendrimers can be internalized into cells
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PAMAM dendrimers are distinguished by their capacity for functionalization, which enhances the properties of the compounds they transport, rendering them highly versatile nanoparticles with extensive applications in the biomedical domain, including drug, vaccine, and gene delivery. These dendrimers can be internalized into cells through various endocytic mechanisms, such as passive diffusion, clathrin-mediated endocytosis, and caveolae-mediated endocytosis, allowing them to traverse the cytoplasm and reach intracellular targets, such as the mitochondria or nucleus. Despite the significant challenge posed by the cytotoxicity of these nanoparticles, which is contingent upon the dendrimer size, surface charge, and generation, numerous strategies have been documented to modify the dendrimer surface using polyethylene glycol and other chemical groups to temporarily mitigate their cytotoxic effects. The potential of PAMAM dendrimers in cancer therapy and other biomedical applications is substantial, owing to their ability to enhance bioavailability, pharmacokinetics, and pharmacodynamics of active ingredients within the body. This underscores the necessity for further investigation into the optimization of internalization pathways and cytotoxicity of these nanoparticles. This review offers a comprehensive synthesis of the current literature on the diverse cellular internalization pathways of PAMAM dendrimers and their cargo molecules, emphasizing the mechanisms of entry, intracellular trafficking, and factors influencing these processes.
Full article
(This article belongs to the Special Issue Biomedical Applications: Advances in Bioengineering and Drug Delivery)
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Open AccessArticle
Triple-Loaded Nanoemulsions Incorporating Coffee Extract for the Photoprotection of Curcumin and Capsaicin: Experimental and Computational Evaluation
by
Nuttapol Boonrueang, Siripat Chaichit, Wipawadee Yooin, Siriporn Okonogi, Kanokwan Kiattisin and Chadarat Ampasavate
Pharmaceutics 2025, 17(7), 926; https://doi.org/10.3390/pharmaceutics17070926 - 17 Jul 2025
Abstract
Background/Objectives: This study aims to present a strategic approach to enhancing the photostability and antioxidative resilience of curcumin and capsaicin by integrating selected natural stabilizers within a nanoemulsion-based delivery system. Methods: Coffee extract (Coffea arabica Linn.), along with its active
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Background/Objectives: This study aims to present a strategic approach to enhancing the photostability and antioxidative resilience of curcumin and capsaicin by integrating selected natural stabilizers within a nanoemulsion-based delivery system. Methods: Coffee extract (Coffea arabica Linn.), along with its active components and vitamin E-containing natural oils, was assessed in terms of improving the photostabilizing and antioxidative retention abilities of curcumin and capsaicin. An optimized ratio of the active mixture was then loaded into a nanoformulation. Results: The analysis of active contents with validated high-performance liquid chromatography (HPLC), ferric reducing antioxidant power (FRAP), and 2,2-diphenyl-1-picrylhydrazyl (DPPH) assays confirmed the stabilization enhancement after irradiation with UV and white light for 72,000–84,000 lux hours. The optimized combination of coffee extract with turmeric and chili mixtures loaded into the optimized nanoemulsion enhanced the half-lives (T1/2) of curcumin and capsaicin by 416% and 390%, respectively. The interactions of curcumin and capsaicin with caffeine and chlorogenic acid were elucidated using computational calculations. Interaction energies (Eint), HOMO-LUMO energy gap (HLG) analysis, and global reactivity descriptors revealed hydrogen bonding interactions be-tween capsaicin and chlorogenic acid, as well as between curcumin and caffeine. Conclusions: By leveraging the synergistic antioxidative properties of coffee extract and vitamin E within a nanoemulsion matrix, this study overcomes the intrinsic stability limitations of curcumin and capsaicin, offering a robust platform for future pharmaceutical and nutraceutical applications.
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(This article belongs to the Special Issue Regenerative Biomaterials with Plant Derivatives for Skin Wound Therapy)
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Clove Oil-Based Nanoemulsion Containing Amphotericin B as a Therapeutic Approach to Combat Fungal Infections
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Marcel Lucas de Almeida, Ana Paula dos Santos Matos, Veronica da Silva Cardoso, Tatielle do Nascimento, Ralph Santos-Oliveira, Leandro Machado Rocha, Francisco Paiva Machado, Franklin Chimaobi Kenechukwu, Alane Beatriz Vermelho and Eduardo Ricci-Júnior
Pharmaceutics 2025, 17(7), 925; https://doi.org/10.3390/pharmaceutics17070925 - 17 Jul 2025
Abstract
Background/Objectives: Candidiasis, primarily caused by Candida albicans, and sporotrichosis, mainly caused by Sporothrix schenckii, are skin fungal infections that pose serious threats to global health. The Candida auris is a great concern in immunocompromised individuals, and while Sporothrix brasiliensis cause sporotrichosis,
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Background/Objectives: Candidiasis, primarily caused by Candida albicans, and sporotrichosis, mainly caused by Sporothrix schenckii, are skin fungal infections that pose serious threats to global health. The Candida auris is a great concern in immunocompromised individuals, and while Sporothrix brasiliensis cause sporotrichosis, an infection commonly found in cats, this disease can be transmitted to humans through scratches or bites. Existing treatments for these fungal infections often cause problems related to resistance and significant side effects. Consequently, development of alternative therapeutic approaches such as nanotechnology-based topical lipid-based formulations is interesting. Thus, the objectives of this study were to prepare clove oil (CO)-in-water nanoemulsions (NEs) containing amphotericin B (AmB) and characterize them with respect to stability, release profile, and in vitro cytotoxic activity against Candida and Sporothrix strains. As a future alternative for the treatment of fungal skin diseases. Methods: Chemical analysis of clove oil was obtained by GC-MS. The NEs were produced using an ultrasound (sonicator) method with varying proportions of CO, Pluronic® F-127, and AmB. The NEs were characterized by droplet size, morphology, stability and in vitro release profile. The antifungal and cytotoxic activity against C. albicans, C. auris, S. schenckii, and S. brasiliensis were ascertained employing agar diffusion and colorimetric MTT assay methods. A checkerboard assay was carried out using clove oil and amphotericin B against C. auris. Results: Eugenol was the major compound identified in CO at a concentration of 80.09%. AmB-loaded NEs exhibited particle sizes smaller than 50 nm and a polydispersity index below 0.25. The optimal Ne (NEMLB-05) remained stable after 150 days of storage at 4 °C. It exhibited rapid release within the first 24 h, followed by a slow and controlled release up to 96 h. NEMLB-05 more effectively inhibited C. auris compared to free AmB and also demonstrated greater activity against C. albicans, S. schenckii, and S. brasiliensis. Clove oil and amphotericin B presented synergism inhibiting the growth of C. auris. Conclusions: The selected CO-in-water NEs containing AmB demonstrated promising potential as a topical therapeutic alternative for treating fungal infections.
Full article
(This article belongs to the Special Issue Nanotechnology in the Treatment of Neglected Parasitic Diseases)
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Open AccessArticle
In Vitro Oral Cavity Permeability Assessment to Enable Simulation of Drug Absorption
by
Pankaj Dwivedi, Priyata Kalra, Haiying Zhou, Khondoker Alam, Eleftheria Tsakalozou, Manar Al-Ghabeish, Megan Kelchen and Giovanni M. Pauletti
Pharmaceutics 2025, 17(7), 924; https://doi.org/10.3390/pharmaceutics17070924 - 17 Jul 2025
Abstract
Background/Objectives: The oral cavity represents a convenient route of administration for drugs that exhibit significant hepatic first-pass extraction. In this study, the mucosal permeation properties of selected active pharmaceutical ingredients (APIs) incorporated into oral cavity drug products that are approved by the U.S.
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Background/Objectives: The oral cavity represents a convenient route of administration for drugs that exhibit significant hepatic first-pass extraction. In this study, the mucosal permeation properties of selected active pharmaceutical ingredients (APIs) incorporated into oral cavity drug products that are approved by the U.S. Food and Drug Administration were quantified using the human-derived sublingual HO-1-u-1 and buccal EpiOral™ in vitro tissue models. Methods: Epithelial barrier properties were monitored using propranolol and Lucifer Yellow as prototypic transcellular and paracellular markers. APIs were dissolved in artificial saliva, pH 6.7, and transepithelial flux from the apical to the basolateral compartment was quantified using HPLC. Results: Apparent permeability coefficients (Papp) calculated for these APIs in the sublingual HO-1-u-1 tissue model varied from Papp = 2.72 ± 0.06 × 10−5 cm/s for asenapine to Papp = 6.21 ± 2.60 × 10−5 cm/s for naloxone. In contrast, the buccal EpiOral™ tissue model demonstrated greater discrimination power in terms of permeation properties for the same APIs, with values ranging from Papp = 3.31 ± 0.83 × 10−7 cm/s for acyclovir to Papp = 2.56 ± 0.68 × 10−5 cm/s for sufentanil. The tissue-associated dose fraction recovered at the end of the transport experiment was significantly increased in the buccal EpiOral™ tissue model, reaching up to 8.5% for sufentanil. Conclusions: Experimental permeation data collected for selected APIs in FDA-approved oral cavity products will serve as a training set to aid the development of predictive computational models for improving algorithms that describe drug absorption from the oral cavity. Following a robust in vitro–in vivo correlation analysis, it is expected that such innovative in silico modeling strategies will the accelerate development of generic oral cavity products by facilitating the utility of model-integrated evidence to support decision making in generic drug development and regulatory approval.
Full article
(This article belongs to the Special Issue Next-Generation Biomaterials for Oral Healthcare: Focus on Regenerative and Delivery Functions)
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Open AccessReview
Tyrosine Kinase Inhibitors for Gastrointestinal Stromal Tumor After Imatinib Resistance
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Xian-Hao Xiao, Qian-Shi Zhang, Ji-Yuan Hu, Yin-Xu Zhang and He Song
Pharmaceutics 2025, 17(7), 923; https://doi.org/10.3390/pharmaceutics17070923 - 17 Jul 2025
Abstract
Gastrointestinal stromal tumors (GISTs) are the most common mesenchymal tumors of the gastrointestinal tract, primarily driven by activating mutations in KIT (CD117) and platelet-derived growth factor receptor alpha (PDGFRA). The introduction of tyrosine kinase inhibitors (TKIs), especially imatinib, has significantly transformed GIST treatment.
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Gastrointestinal stromal tumors (GISTs) are the most common mesenchymal tumors of the gastrointestinal tract, primarily driven by activating mutations in KIT (CD117) and platelet-derived growth factor receptor alpha (PDGFRA). The introduction of tyrosine kinase inhibitors (TKIs), especially imatinib, has significantly transformed GIST treatment. However, the emergence of both primary and secondary resistance to imatinib presents ongoing therapeutic challenges. This review comprehensively explores the mechanisms underlying imatinib resistance and evaluates subsequent TKI therapies. Sunitinib, regorafenib, and ripretinib are currently approved as standard second-, third-, and fourth-line therapies, each demonstrating efficacy against distinct mutational profiles. Avapritinib, notably effective against PDGFRA D842V mutations, represents a milestone for previously untreatable subgroups. Several alternative agents—such as nilotinib, masitinib, sorafenib, dovitinib, pazopanib, and ponatinib—have shown varying degrees of success in refractory cases or specific genotypes. Investigational compounds, including crenolanib, bezuclastinib, famitinib, motesanib, midostaurin, IDRX-42, and olverembatinib, are under development to address resistant or wild-type GISTs. Despite progress, long-term efficacy remains limited due to evolving resistance. Future strategies include precision medicine approaches such as ctDNA-guided therapy, rational drug combinations, and novel drug delivery systems to optimize bioavailability and reduce toxicity. Ongoing research will be crucial for refining treatment sequencing and expanding therapeutic options, especially for rare GIST subtypes.
Full article
(This article belongs to the Special Issue Kinase Inhibitor for Cancer Therapy, 2nd Edition)
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Open AccessArticle
Development of Co-Amorphous Systems for Inhalation Therapy—Part 1: From Model Prediction to Clinical Success
by
Eleonore Fröhlich, Aurora Bordoni, Nila Mohsenzada, Stefan Mitsche, Hartmuth Schröttner and Sarah Zellnitz-Neugebauer
Pharmaceutics 2025, 17(7), 922; https://doi.org/10.3390/pharmaceutics17070922 - 16 Jul 2025
Abstract
Background/Objectives: The integration of machine learning (ML) and artificial intelligence (AI) has revolutionized the pharmaceutical industry by improving drug discovery, development and manufacturing processes. Based on literature data, an ML model was developed by our group to predict the formation of binary
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Background/Objectives: The integration of machine learning (ML) and artificial intelligence (AI) has revolutionized the pharmaceutical industry by improving drug discovery, development and manufacturing processes. Based on literature data, an ML model was developed by our group to predict the formation of binary co-amorphous systems (COAMSs) for inhalation therapy. The model’s ability to develop a dry powder formulation with the necessary properties for a predicted co-amorphous combination was evaluated. Methods: An extended experimental validation of the ML model by co-milling and X-ray diffraction analysis for 18 API-API (active pharmaceutical ingredient) combinations is presented. Additionally, one COAMS of rifampicin (RIF) and ethambutol (ETH), two first-line tuberculosis (TB) drugs are developed further for inhalation therapy. Results: The ML model has shown an accuracy of 79% in predicting suitable combinations for 35 APIs used in inhalation therapy; experimental accuracy was demonstrated to be 72%. The study confirmed the successful development of stable COAMSs of RIF-ETH either via spray-drying or co-milling. In particular, the milled COAMSs showed better aerosolization properties (higher ED and FPF with lower standard deviation). Further, RIF-ETH COAMSs show much more reproducible results in terms of drug quantity dissolved over time. Conclusions: ML has been shown to be a suitable tool to predict COAMSs that can be developed for TB treatment by inhalation to save time and cost during the experimental screening phase.
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(This article belongs to the Special Issue New Platform for Tuberculosis Treatment)
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Open AccessArticle
The Development of a Multilayer Transdermal Patch Platform Based on Electrospun Nanofibers for the Delivery of Caffeine
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Jorge Teno, Zoran Evtoski, Cristina Prieto and Jose M. Lagaron
Pharmaceutics 2025, 17(7), 921; https://doi.org/10.3390/pharmaceutics17070921 - 16 Jul 2025
Abstract
Background/Objectives: The work presented herein focused on the development and characterization of a transdermal caffeine platform fabricated from ultrathin micro- and submicron fibers produced via electrospinning. Methods: The formulations incorporated caffeine encapsulated in a polyethylene oxide (PEO) matrix, combined with various
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Background/Objectives: The work presented herein focused on the development and characterization of a transdermal caffeine platform fabricated from ultrathin micro- and submicron fibers produced via electrospinning. Methods: The formulations incorporated caffeine encapsulated in a polyethylene oxide (PEO) matrix, combined with various permeation enhancers. A backing layer made of annealed electrospun polycaprolactone (PCL) facilitated the lamination of the two layers to form the final multilayer patch. Comprehensive characterization was conducted, utilizing scanning electron microscopy (SEM) to assess the fiber morphology, attenuated total reflectance Fourier transform infrared spectroscopy (ATR-FTIR) for chemical detection and to assess the stability of the caffeine, and differential scanning calorimetry (DSC) along with wide-angle X-ray scattering (WAXS) to analyze the physical state of the caffeine within the fibers of the active layer. Additionally, Franz cell permeation studies were performed using both synthetic membranes (Strat-M) and ex vivo human stratum corneum (SC) to evaluate and model the permeation kinetics. Results: These experiments demonstrated the significant role of enhancers in modulating the caffeine permeation rates provided by the patch, achieving permeation rates of up to 0.73 mg/cm2 within 24 h. Conclusions: This work highlights the potential of using electro-hydrodynamic processing technology to develop innovative transdermal delivery systems for drugs, offering a promising strategy for enhancing efficacy and innovative therapeutic direct plasma administration.
Full article
(This article belongs to the Special Issue Dermal and Transdermal Drug Delivery Systems)
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Synthesis and Evaluation of [18F]AlF-NOTA-iPD-L1 as a Potential Theranostic Pair for [177Lu]Lu-DOTA-iPD-L1
by
Guillermina Ferro-Flores, Myrna Luna-Gutiérrez, Blanca Ocampo-García, Nallely Jiménez-Mancilla, Nancy Lara-Almazán, Rigoberto Oros-Pantoja, Clara Santos-Cuevas, Erika Azorín-Vega and Laura Meléndez-Alafort
Pharmaceutics 2025, 17(7), 920; https://doi.org/10.3390/pharmaceutics17070920 - 16 Jul 2025
Abstract
Background/Objective: Programmed cell death ligand-1 (PD-L1), which is overexpressed in certain tumors, inhibits the body’s natural immune response by providing an “off” signal that enables cancer cells to evade the immune system. It has been demonstrated that [177Lu]Lu-DOTA-iPD-L1 (PD-L1 inhibitor
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Background/Objective: Programmed cell death ligand-1 (PD-L1), which is overexpressed in certain tumors, inhibits the body’s natural immune response by providing an “off” signal that enables cancer cells to evade the immune system. It has been demonstrated that [177Lu]Lu-DOTA-iPD-L1 (PD-L1 inhibitor cyclic peptide) promotes immune responses. This study aimed to synthesize and evaluate [18F]AlF-NOTA-iPD-L1 as a novel radiotracer for PD-L1 positron emission tomography (PET) imaging and as a potential theranostic pair for [177Lu]Lu-DOTA-iPD-L1. Methods: The NOTA-iPD-L1 peptide conjugate was synthesized and characterized by U.V.-vis, I.R.-FT, and UPLC-mass spectroscopies. Radiolabeling was performed using [18F]AlF as the precursor, and the radiochemical purity (HPLC), partition coefficient, and serum stability were assessed. Cellular uptake and internalization (in 4T1 triple-negative breast cancer cells), binding competition, immunofluorescence, and Western blot assays were applied for the radiotracer in vitro characterization. Biodistribution in mice bearing 4T1 tumors was performed, and molecular imaging (Cerenkov images) of [18F]AlF-NOTA-iPD-L1 and [177Lu]Lu-DOTA-iPD-L1 in the same mouse was obtained. Results: [18F]AlF-NOTA-iPD-L1 was prepared with a radiochemical purity greater than 97%, and it demonstrated high in vitro and in vivo stability, as well as specific recognition by the PD-L1 protein (IC50 = 9.27 ± 2.69 nM). Biodistribution studies indicated a tumor uptake of 6.4% ± 0.9% ID/g at 1-hour post-administration, and Cerenkov images showed a high tumor uptake of both [18F]AlF-NOTA-iPD-L1 and 177Lu-iPD-L1 in the same mouse. Conclusions: These results warrant further studies to evaluate the clinical usefulness of [18F]AlF-NOTA-iPD-L1/[177Lu]Lu-DOTA-iPD-L1 as a radiotheranostic pair in combination with anti-PD-L1/PD1 immunotherapy.
Full article
(This article belongs to the Special Issue Advances in Radiopharmaceuticals: Enhancing Targeted Delivery, Disease Diagnosis, and Therapeutic Applications)
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Quantification of Total and Unbound Selinexor Concentrations in Human Plasma by a Fully Validated Liquid Chromatography-Tandem Mass Spectrometry Method
by
Suhyun Lee, Seungwon Yang, Hyeonji Kim, Wang-Seob Shim, Eunseo Song, Seunghoon Han, Sung-Soo Park, Suein Choi, Sungpil Han, Sung Hwan Joo, Seok Jun Park, Beomjin Shin, Donghyun Kim, Hyeon Su Kim, Kyung-Tae Lee and Eun Kyoung Chung
Pharmaceutics 2025, 17(7), 919; https://doi.org/10.3390/pharmaceutics17070919 - 16 Jul 2025
Abstract
Background/Objectives: Selinexor is a selective nuclear-export inhibitor approved for hematologic malignancies, characterized by extensive plasma protein binding (>95%). However, a validated analytical method to accurately measure the clinically relevant unbound fraction of selinexor in human plasma has not yet been established. This study
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Background/Objectives: Selinexor is a selective nuclear-export inhibitor approved for hematologic malignancies, characterized by extensive plasma protein binding (>95%). However, a validated analytical method to accurately measure the clinically relevant unbound fraction of selinexor in human plasma has not yet been established. This study aimed to develop a fully validated bioanalytical assay for simultaneous quantification of total and unbound selinexor concentrations in human plasma. Methods: We established and fully validated an analytical method based on liquid chromatography–tandem mass spectrometry (LC-MS/MS) capable of quantifying total and unbound selinexor concentrations in human plasma. Unbound selinexor was separated using ultrafiltration, and selinexor was efficiently extracted from 50 μL of plasma by liquid–liquid extraction. Chromatographic separation was achieved on a C18 column using an isocratic mobile phase (0.1% formic acid:methanol, 12:88 v/v) with a relatively short runtime of 2.5 min. Results: Calibration curves showed excellent linearity over a range of 5–2000 ng/mL for total selinexor (r2 ≥ 0.998) and 0.05–20 ng/mL for unbound selinexor (r2 ≥ 0.995). The precision (%CV ≤ 10.35%) and accuracy (92.5–104.3%) for both analytes met the regulatory criteria. This method successfully quantified selinexor in plasma samples from renally impaired patients with multiple myeloma, demonstrating potential inter-individual differences in unbound drug concentrations. Conclusions: This validated bioanalytical assay enables precise clinical pharmacokinetic assessments in a short runtime using a small plasma volume and, thus, assists in individualized dosing of selinexor, particularly for renally impaired patients with altered protein binding.
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(This article belongs to the Section Pharmacokinetics and Pharmacodynamics)
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Ferroptosis Among the Antiproliferative Pathways Activated by a Lipophilic Ruthenium(III) Complex as a Candidate Drug for Triple-Negative Breast Cancer
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Maria Grazia Ferraro, Federica Iazzetti, Marco Bocchetti, Claudia Riccardi, Daniela Montesarchio, Rita Santamaria, Gabriella Misso, Marialuisa Piccolo and Carlo Irace
Pharmaceutics 2025, 17(7), 918; https://doi.org/10.3390/pharmaceutics17070918 - 16 Jul 2025
Abstract
Background/Objectives: In the context of preclinical studies, we have hitherto showcased that a low-molecular-weight ruthenium(III) complex we named AziRu holds significant potential for further developments as an anticancer candidate drug. When appropriately converted into stable nanomaterials and delivered into tumor cells, AziRu
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Background/Objectives: In the context of preclinical studies, we have hitherto showcased that a low-molecular-weight ruthenium(III) complex we named AziRu holds significant potential for further developments as an anticancer candidate drug. When appropriately converted into stable nanomaterials and delivered into tumor cells, AziRu exhibits superior antiproliferative activity, benefiting from a multimodal mechanism of action. The activation of regulated cell death (RCD) pathways (i.e., apoptosis and autophagy) has been proved in metastatic phenotypes, including triple-negative breast cancer (TNBC) cells. This study focuses on a bioengineered lipophilic derivative of AziRu, named PalmiPyRu, that we are currently developing as a potential anticancer drug in preclinical studies. When delivered in this way, AziRu confirms a multimodal mechanism of action in effectively blocking the growth and proliferation of TNBC phenotypes. Special focus is reserved for the activation of the ferroptotic pathway as a consequence of redox imbalance and interference with iron homeostasis, as well as the glutathione biosynthetic pathway. Methods: Human preclinical models of specific TNBC phenotypes and healthy cell cultures of different histological origin were selected. After in vitro treatments, cellular responses were carefully analyzed, and targeted biochemical and molecular biology experiments coupled to confocal microscopy allowed us to explore the antiproliferative effects of PalmiPyRu. Results: In this study, we unveil that PalmiPyRu can enter TNBC cells and interfere with both the iron homeostasis and the cystine-glutamate antiporter system Xc-, causing significant oxidative stress and the accumulation of lipid oxidation products. The increase in intracellular reactive free iron and depletion of glutathione engender a lethal condition, driving cancer cells toward the activation of ferroptosis. Conclusions: Overall, these outcomes allow us, for the first time, to couple the antiproliferative effect of a ruthenium-based candidate drug with the inhibition of the Xc- antiporter system and Fenton chemistry, thereby branding PalmiPyRu as an effective multimodal inducer of ferroptosis. Molecular mechanisms of action deserve further investigations, and new studies are underway to uncover how interference with Xc- controls cell fate, allowing us to explore the connection between iron metabolism regulation, oxidative stress and RCD pathways activation.
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(This article belongs to the Section Drug Targeting and Design)
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Recent Advances in the Use of Ganoderma lucidum and Coriolus versicolor Mushrooms to Enhance the Anticancer Efficacy of EGFR-Targeted Drugs in Lung Cancer
by
Hang Zhang, Longling Wang, Yuet Wa Chan, William C. Cho, Zhong Zuo and Kenneth K. W. To
Pharmaceutics 2025, 17(7), 917; https://doi.org/10.3390/pharmaceutics17070917 - 15 Jul 2025
Abstract
Lung cancer is the leading cause of cancer-related deaths worldwide. Non-small cell lung cancer (NSCLC) is the major subtype, accounting for more than 85% of all lung cancer cases. Recent advances in precision oncology have allowed NSCLC patients bearing specific oncogenic epidermal growth
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Lung cancer is the leading cause of cancer-related deaths worldwide. Non-small cell lung cancer (NSCLC) is the major subtype, accounting for more than 85% of all lung cancer cases. Recent advances in precision oncology have allowed NSCLC patients bearing specific oncogenic epidermal growth factor receptor (EGFR) mutations to respond well to EGFR tyrosine kinase inhibitors (TKIs). Due to the high EGFR mutation frequency (up to more than 50%) observed particularly in Asian NSCLC patients, EGFR-TKIs have produced unprecedented clinical responses. Depending on their binding interactions with EGFRs, EGFR-TKIs are classified as reversible (first-generation: gefitinib and erlotinib) or irreversible inhibitors (second-generation: afatinib and dacomitinib; third-generation: osimertinib). While the discovery of osimertinib represents a breakthrough in the treatment of NSCLC, most patients eventually relapse and develop drug resistance. Novel strategies to overcome osimertinib resistance are urgently needed. In Asian countries, the concomitant use of Western medicine and traditional Chinese medicine (TCM) is very common. Ganoderma lucidum (Lingzhi) and Coriolus versicolor (Yunzhi) are popular TCMs that are widely consumed by cancer patients to enhance anticancer efficacy and alleviate the side effects associated with cancer therapy. The bioactive polysaccharides and triterpenes in these medicinal mushrooms are believed to contribute to their anticancer and immunomodulating effects. This review presents the latest update on the beneficial combination of Lingzhi/Yunzhi and EGFR-TKIs to overcome drug resistance. The effects of Lingzhi/Yunzhi on various oncogenic signaling pathways and anticancer immunity, as well as their potential to overcome EGFR-TKI resistance, are highlighted. The potential risk of herb–drug interactions could become critical when cancer patients take Lingzhi/Yunzhi as adjuvants during cancer therapy. The involvement of drug transporters and cytochrome P450 enzymes in these herb–drug interactions is summarized. Finally, we also discuss the opportunities and future prospects regarding the combined use of Lingzhi/Yunzhi and EGFR-TKIs in cancer patients.
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(This article belongs to the Special Issue Combination Therapy Approaches for Cancer Treatment)
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Open AccessArticle
Microencapsulation of Analgesics as an Analog Form of Medicine
by
Aidana Nakipekova, Bates Kudaibergenova, Arkady S. Abdurashitov and Gleb B. Sukhorukov
Pharmaceutics 2025, 17(7), 916; https://doi.org/10.3390/pharmaceutics17070916 - 15 Jul 2025
Abstract
Objectives: This research focuses on the development of fabrication approaches for microparticles intended for controlled drug delivery. The primary objective is to identify the most suitable polymer type, particle size, and morphology for encapsulating a water-soluble crystalline drug. Optimizing these parameters may enhance
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Objectives: This research focuses on the development of fabrication approaches for microparticles intended for controlled drug delivery. The primary objective is to identify the most suitable polymer type, particle size, and morphology for encapsulating a water-soluble crystalline drug. Optimizing these parameters may enhance structural stability and prolong the release of this active substance. Methods: The microparticles were fabricated through the encapsulation of a drug substance within a polymer carrier and employing polymer casting on prepatterned surfaces, followed by the loading of drug precipitates and the application of a sealing layer. The crystalline powder 1-allyl-2,5-dimethylpiperidol-4 hydrochloride served as the core cargo material, while the walls of these particles were composed of polylactic acid (PLA) and a poly (α-caprolactone) (PCL) in a 70:30 composition ratio. Results: The size and volume of the microparticles were found to be dependent on the geometric parameters of the template and the concentration of the polymer solutions. The study demonstrates the formation, physical dimensions, and particle count at varied polymer compositions and concentrations. The formation of the PLA and PCL mixture occurred solely through physical interactions. Scanning electron microscopy (SEM) and optical microscopy were employed to observe the appearance and physical dimensions of the microparticles. The obtained data confirm that tailored polymer compositions can yield consistent particle morphology and a suitable drug elution rate. Conclusions: The results indicate that microparticles sealed with an optimal polymer composition exhibit enhanced release properties. This finding highlights the feasibility of microencapsulation at precise ratios and concentrations of polymers to achieve the long-lasting effects of water-soluble drugs.
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(This article belongs to the Special Issue Multifunctional Nanomaterials in Drug Delivery)
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Pharmacokinetics of Pegaspargase with a Limited Sampling Strategy for Asparaginase Activity Monitoring in Children with Acute Lymphoblastic Leukemia
by
Cristina Matteo, Antonella Colombini, Marta Cancelliere, Tommaso Ceruti, Ilaria Fuso Nerini, Luca Porcu, Massimo Zucchetti, Daniela Silvestri, Maria Grazia Valsecchi, Rosanna Parasole, Luciana Vinti, Nicoletta Bertorello, Daniela Onofrillo, Massimo Provenzi, Elena Chiocca, Luca Lo Nigro, Laura Rachele Bettini, Giacomo Gotti, Silvia Bungaro, Martin Schrappe, Paolo Ubezio and Carmelo Rizzariadd
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Pharmaceutics 2025, 17(7), 915; https://doi.org/10.3390/pharmaceutics17070915 - 15 Jul 2025
Abstract
Background: Asparaginase (ASPase) plays an important role in the therapy of acute lymphoblastic leukemia (ALL). Serum ASPase activity (SAA) can be modified and even abolished by host immune responses; therefore, current treatment guidelines recommend to monitor SAA during treatment administration. The SAA
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Background: Asparaginase (ASPase) plays an important role in the therapy of acute lymphoblastic leukemia (ALL). Serum ASPase activity (SAA) can be modified and even abolished by host immune responses; therefore, current treatment guidelines recommend to monitor SAA during treatment administration. The SAA monitoring schedule needs to be carefully planned to reduce the number of samples without hampering the possibility of measuring pharmacokinetics (PK) parameters in individual patients. Complex modelling approaches, not easily applicable in common practice, have been applied in previous studies to estimate ASPase PK parameters. This study aimed to estimate PK parameters by using a simplified approach suitable for real-world settings with limited sampling. Methods: Our study was based on 434 patients treated in Italy within the AIEOP-BFM ALL 2009 trial. During the induction phase, patients received two doses of pegylated ASPase and were monitored with blood sampling at five time points, including time 0. PK parameters were estimated by using the individually available SAA measurements with simple modifications of the classical non-compartmental PK analysis. We also took the opportunity to develop and validate a series of limited sampling models to predict ASPase exposure. Results: During the induction phase, average ASPase activity at day 7 was 1380 IU/L after the first dose and 1948 IU/L after the second dose; therapeutic SAA levels (>100 IU/L) were maintained until day 33 in 90.1% of patients. The average AUC and clearance were 46,937 IU/L × day and 0.114 L/day/m2, respectively. The database was analyzed for possible associations of PK parameters with biological characteristics of the patients, finding only a limited dependence on sex, age and risk score; however, these differences were not sufficient to allow any dose or schedule adjustments. Thereafter the possibility of further sampling reduction by using simple linear models to estimate the AUC was also explored. The most simple model required only two samplings 7 days after each ASPase dose, with the AUC being proportional to the sum of the two measured activities A(7) and A(21), calculated by the formula AUC = 14.1 × [A(7) + A(21)]. This model predicts the AUC with 6% average error and 35% maximum error compared to the AUC estimated with all available measures. Conclusions: Our study demonstrates the feasibility of a direct estimation of PK parameters in a real-life situation with limited and variable blood sampling schedules and also offers a simplified method and formulae easily applicable in clinical practice while maintaining a reliable pharmacokinetic monitoring.
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(This article belongs to the Section Pharmacokinetics and Pharmacodynamics)
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Physiologically Based Pharmacokinetic Simulation of Tofacitinib in Humans Using Extrapolation from Single-Species Renal Failure Model
by
Sung Hun Bae, So Yeon Park, Hyeon Gyeom Choi and So Hee Kim
Pharmaceutics 2025, 17(7), 914; https://doi.org/10.3390/pharmaceutics17070914 - 15 Jul 2025
Abstract
Background/Objectives: Tofacitinib is a Janus kinase 1 and 3 inhibitor that was developed to treat rheumatoid arthritis. Accordingly, this study aimed to predict plasma tofacitinib concentrations and pharmacokinetic parameters in patients with renal failure through physiologically based pharmacokinetic (PBPK) simulations. Methods: PK-Sim
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Background/Objectives: Tofacitinib is a Janus kinase 1 and 3 inhibitor that was developed to treat rheumatoid arthritis. Accordingly, this study aimed to predict plasma tofacitinib concentrations and pharmacokinetic parameters in patients with renal failure through physiologically based pharmacokinetic (PBPK) simulations. Methods: PK-Sim and Simcyp simulators were used, as well as conventional Dedrick plot analysis, employing a single animal extrapolation method. The predictions were compared with previously published data. Results: PBPK simulations of tofacitinib in patients with renal failure closely matched the observed plasma concentration profiles and pharmacokinetic results, including the area under the plasma concentration–time curve (AUC), maximum plasma concentration (Cmax), and time to reach Cmax (Tmax). The ratios of the simulated to observed plasma concentrations and pharmacokinetic parameters for tofacitinib were within a 0.5–2.0-fold error range. Although the results from the Dedrick plot were reasonably good, they were less accurate than those of the PBPK simulations. This was because the Dedrick plot relied solely on preclinical plasma concentration data without incorporating drug physicochemical properties, in vitro data, or physiological and pathophysiological variables. Conclusions: The findings suggest that PBPK simulations using single-species extrapolation effectively provide preliminary estimates of plasma tofacitinib concentration profiles and pharmacokinetic parameters in humans under specific conditions, including renal failure. Furthermore, the results provide a foundation for adjusting tofacitinib dosage and dosing schedules to maintain effective plasma concentrations by considering the pathophysiological characteristics of patients according to their specific diseases.
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(This article belongs to the Special Issue Advances in Physiologically Based Pharmacokinetic (PBPK) Modeling and Applications)
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Pharmacokinetic Adaptations in Pregnancy: Implications for Optimizing Antiretroviral Therapy in HIV-Positive Women
by
Natalia Briceño-Patiño, María Camila Prieto, Paula Manrique, Carlos-Alberto Calderon-Ospina and Leonardo Gómez
Pharmaceutics 2025, 17(7), 913; https://doi.org/10.3390/pharmaceutics17070913 - 15 Jul 2025
Abstract
Pregnancy introduces significant physiological changes that alter the pharmacokinetics (PK) of antiretroviral therapy (ART), impacting its safety and efficacy in HIV-positive women. Optimizing ART during pregnancy is critical to maintaining maternal virological suppression and preventing mother-to-child transmission (MTCT) of HIV. This review evaluates
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Pregnancy introduces significant physiological changes that alter the pharmacokinetics (PK) of antiretroviral therapy (ART), impacting its safety and efficacy in HIV-positive women. Optimizing ART during pregnancy is critical to maintaining maternal virological suppression and preventing mother-to-child transmission (MTCT) of HIV. This review evaluates the impact of pregnancy-induced PK changes on ART and proposes strategies for tailored regimens to improve outcomes. A comprehensive review of published literature was conducted, focusing on PK adaptations during pregnancy and their implications for different ART classes, including protease inhibitors (PIs), integrase strand transfer inhibitors (INSTIs), and nucleoside reverse transcriptase inhibitors (NRTIs). Key studies were analyzed to assess drug exposure, efficacy, and safety. Pregnancy significantly alters the PK of antiretrovirals, with increased hepatic metabolism, renal clearance, and changes in plasma protein binding leading to reduced drug exposure. For example, drugs like lopinavir and atazanavir require dose adjustments, while dolutegravir maintains efficacy despite reduced plasma levels. Integrase inhibitors demonstrate favorable virological suppression, although cobicistat-boosted regimens show subtherapeutic levels. Tailored approaches, such as therapeutic drug monitoring (TDM), optimize ART efficacy while minimizing toxicity. Pregnancy-specific PK changes necessitate evidence-based ART adjustments to ensure virological suppression and reduce MTCT risk. Incorporating TDM, leveraging pharmacogenomic insights, and prioritizing maternal and neonatal safety are critical for personalized ART management. Further research into long-acting formulations and global guideline harmonization is needed to address disparities in care and improve outcomes for HIV-positive pregnant women.
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(This article belongs to the Special Issue Pharmacokinetics of Drugs in Pregnancy and Lactation)
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Nanoradiopharmaceuticals: Design Principles, Radiolabeling Strategies, and Biomedicine Applications
by
Andrés Núñez-Salinas, Cristian Parra-Garretón, Daniel Acuña, Sofía Peñaloza, Germán Günther, Soledad Bollo, Francisco Arriagada and Javier Morales
Pharmaceutics 2025, 17(7), 912; https://doi.org/10.3390/pharmaceutics17070912 - 14 Jul 2025
Abstract
Nanoradiopharmaceuticals integrate nanotechnology with nuclear medicine to enhance the precision and effectiveness of radiopharmaceuticals used in diagnostic imaging and targeted therapies. Nanomaterials offer improved targeting capabilities and greater stability, helping to overcome several limitations. This review presents a comprehensive overview of the fundamental
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Nanoradiopharmaceuticals integrate nanotechnology with nuclear medicine to enhance the precision and effectiveness of radiopharmaceuticals used in diagnostic imaging and targeted therapies. Nanomaterials offer improved targeting capabilities and greater stability, helping to overcome several limitations. This review presents a comprehensive overview of the fundamental design principles, radiolabeling techniques, and biomedical applications of nanoradiopharmaceuticals, with a particular focus on their expanding role in precision oncology. It explores key areas, including single- and multi-modal imaging modalities (SPECT, PET), radionuclide therapies involving beta, alpha, and Auger emitters, and integrated theranostic systems. A diverse array of nanocarriers is examined, including liposomes, micelles, albumin nanoparticles, PLGA, dendrimers, and gold, iron oxide, and silica-based platforms, with an assessment of both preclinical and clinical research outcomes. Theranostic nanoplatforms, which integrate diagnostic and therapeutic functions within a single system, enable real-time monitoring and personalized dose optimization. Although some of these systems have progressed to clinical trials, several obstacles remain, including formulation stability, scalable manufacturing, regulatory compliance, and long-term safety considerations. In summary, nanoradiopharmaceuticals represent a promising frontier in personalized medicine, particularly in oncology. By combining diagnostic and therapeutic capabilities within a single nanosystem, they facilitate more individualized and adaptive treatment approaches. Continued innovation in formulation, radiochemistry, and regulatory harmonization will be crucial to their successful routine clinical use.
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(This article belongs to the Special Issue Nanosystems for Advanced Diagnostics and Therapy)
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