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Search Results (292)

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Keywords = lipid-based nanocarriers

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25 pages, 3149 KB  
Article
Design and Factorial Optimization of Curcumin and Resveratrol Co-Loaded Lipid Nanocarriers for Topical Delivery
by Daniela Pastorim Vaiss, Débora Cristine Chrisostomo Dias, Virginia Campello Yurgel, Fernanda Beatriz Venturi Araujo, Ledilege Cucco Porto, Janaina Fernandes de Medeiros Burkert, Marcelo Augusto Germani Marinho, Daza de Moraes Vaz Batista Filgueira and Cristiana Lima Dora
Pharmaceutics 2026, 18(1), 109; https://doi.org/10.3390/pharmaceutics18010109 - 15 Jan 2026
Viewed by 179
Abstract
Background: Nanotechnology provides innovative strategies to enhance drug delivery and therapeutic efficacy through advanced nanocarrier systems. Objectives: This study aimed to develop and optimize a nanostructured lipid carrier (NLC) co-encapsulating curcumin (CUR) and resveratrol (RESV) using a fractional factorial design to [...] Read more.
Background: Nanotechnology provides innovative strategies to enhance drug delivery and therapeutic efficacy through advanced nanocarrier systems. Objectives: This study aimed to develop and optimize a nanostructured lipid carrier (NLC) co-encapsulating curcumin (CUR) and resveratrol (RESV) using a fractional factorial design to develop a topical formulation with antioxidant and anti-inflammatory properties. Methods: NLCs were produced via hot emulsification followed by high-pressure homogenization, and their physicochemical characteristics, drug content, stability, release profile, antioxidant activity, skin delivery, and cellular compatibility were evaluated. Results: The optimized formulation exhibited an average particle size of approximately 300 nm, a polydispersity index below 0.3, and high drug loading for both compounds. Stability studies over 90 days revealed no significant changes in physicochemical parameters, confirming the formulation’s robustness. In vitro release assays demonstrated sustained release of both actives, with 58.6 ± 2.9% of CUR and 97 ± 3% of RESV released after 72 h. Antioxidant activity, assessed by the DPPH and ABTS assays, showed concentration-dependent radical-scavenging effects, indicating antioxidant potential. Skin permeation/retention experiments using porcine skin showed enhanced retention of CUR and RESV within the tissue, with no detectable permeation, indicating suitability for topical delivery. In addition, in vitro cell assays using human keratinocytes showed concentration-dependent responses and acceptable cellular compatibility. Conclusions: Overall, this study demonstrates the successful application of nanotechnology and experimental design to develop stable and efficient lipid-based nanocarriers containing natural polyphenol for topical therapy targeting oxidative and inflammatory skin disorders. Full article
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24 pages, 3695 KB  
Review
Therapeutic Advances of Curcumin and Nanocurcumin in Glioblastoma: Molecular Targets, Bioavailability, and Drug Delivery
by Md Ataur Rahman, Mahesh Kumar Yadab and Meser M. Ali
Nutrients 2026, 18(2), 194; https://doi.org/10.3390/nu18020194 - 7 Jan 2026
Viewed by 384
Abstract
Glioblastoma (GBM), the most common, invasive, and chemoresistant form of adult primary brain cancer, is characterized by rapid cell proliferation, local invasiveness, and resistance to chemotherapy (e.g., temozolomide (TMZ)) and radiation therapy. Curcumin, a bioactive polyphenol derived from Curcuma longa, has exhibited [...] Read more.
Glioblastoma (GBM), the most common, invasive, and chemoresistant form of adult primary brain cancer, is characterized by rapid cell proliferation, local invasiveness, and resistance to chemotherapy (e.g., temozolomide (TMZ)) and radiation therapy. Curcumin, a bioactive polyphenol derived from Curcuma longa, has exhibited exceptional anti-cancer properties, including anti-proliferative, pro-apoptotic, anti-inflammatory, and anti-angiogenic activities in a wide range of cancer models, including GBM. However, the clinical application of curcumin has been seriously limited by several challenges, including low water solubility, low bioavailability, rapid systemic clearance, and poor blood–brain barrier (BBB) penetration. To overcome these challenges, several nanocarrier systems to produce nanocurcumin have been developed, including liposomes, polymeric nanoparticles, solid lipid nanoparticles, dendrimers, and micelles. These nanoformulations improve the solubility, stability, systemic circulation, and target-directed delivery of curcumin to glioma cells, thereby resulting in a high level of accumulation in the glioma microenvironment. On the other hand, this work is devoted to the potential of curcumin and nanocurcumin for the treatment of GBM. The article provides a detailed review of the major molecular targets of curcumin, such as NF-κB, STAT3, PI3K/AKT/mTOR, and p53 signaling pathways, as well as recent advancements in nanotechnology-based delivery platforms that improve drug delivery across the BBB and their possible clinical translation. We also include a thorough examination of the issues, limitations, and potential opportunities associated with the clinical advancement of curcumin-based therapeutics for GBM. Full article
(This article belongs to the Special Issue Natural Active Substances and Cancer)
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29 pages, 5336 KB  
Review
Lipid-Based Colloidal Nanocarriers for Site-Specific Drug Delivery
by Kamyar Shameli, Behnam Kalali, Hassan Moeini and Aras Kartouzian
Colloids Interfaces 2026, 10(1), 7; https://doi.org/10.3390/colloids10010007 - 4 Jan 2026
Viewed by 553
Abstract
Lipid nanoparticles (LNPs) are now the go-to method for delivering genetic medicines, backed by real-world use in patients. Things like which fats they are made of, their shape at the molecular level, how ingredients mix, and how they are built, matter a lot. [...] Read more.
Lipid nanoparticles (LNPs) are now the go-to method for delivering genetic medicines, backed by real-world use in patients. Things like which fats they are made of, their shape at the molecular level, how ingredients mix, and how they are built, matter a lot. This review attempts to take a close look at how different components, such as ionizable lipids, auxiliary lipids (DSPC, DOPE), cholesterol, and PEG-based lipids, affect the bioavailability of LNPs. It also focuses on key functions of LNPs, including packaging genetic material, escaping cellular traps, spreading in the body, and remaining active in the blood. New data show that lipids with the right handedness and highly sensitive chiroptical quality control can sharpen delivery accuracy and boost transport rates, turning stereochemistry into a practical design knob. Rather than simply listing results, we examine real-world examples that are already used to regulate gene expression, enhance mRNA expression, splenic targeting, and show great potential for gene repair, protein replacement, and DNA base-editing applications. Also, recent advances in AI-based designs for LNPs that take molecular shape into account and help speed up modifications to lipid arrangements and mixture configurations are highlighted. In summary, this paper presents a practical and scientific blueprint to support smarter production of advanced LNPs used in genetic medicine, addressing existing obstacles, balanced with future opportunities. Full article
(This article belongs to the Special Issue Feature Reviews in Colloids and Interfaces)
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18 pages, 315 KB  
Review
Advances in Nanotechnology-Based Topical Delivery Systems for Skincare Applications
by Ziwei Yan, Sunxin Zhang, Guyuan Wu, Yunxiang Kang, Cong Fu, Zihan Wang, Guoqi Wang, Lu Tang and Wei Wang
Pharmaceutics 2026, 18(1), 63; https://doi.org/10.3390/pharmaceutics18010063 - 3 Jan 2026
Viewed by 486
Abstract
The growing demand for effective skincare products that can effectively target specific dermatological concerns has accelerated the development of advanced delivery technologies. Among them, nanocarrier-based topical delivery systems have gained significant attention for their ability to enhance the performance of skincare formulations. Acting [...] Read more.
The growing demand for effective skincare products that can effectively target specific dermatological concerns has accelerated the development of advanced delivery technologies. Among them, nanocarrier-based topical delivery systems have gained significant attention for their ability to enhance the performance of skincare formulations. Acting as versatile delivery tools, nanocarriers not only stabilize and protect sensitive cosmetic ingredients but also improve their penetration through the skin barrier and enable controlled, sustained, or targeted release. Therefore, this review focuses on the recent achievements of nanocarrier-based topical delivery technology for skincare applications, which systematically summarizes the design principles, mechanisms and functional characteristics of diverse nano-based delivery platforms, including vesicular nanocarriers, lipid-based nanocarriers, emulsion-based nanocarriers, polymeric nanocarriers, inorganic nanoparticles, and inclusion complexes. Meanwhile, these nanocarriers are discussed according to their relevance to the pathogenesis of prevalent skin disorders, highlighting how tailored nanocarriers can address specific therapeutic or cosmetic needs. Overall, this review emphasizes the emerging trends and future perspectives of nanotechnology-based topical delivery systems in modern cosmetology, offering more opportunities for precise, effective and science-driven cosmetic solutions. Full article
(This article belongs to the Section Nanomedicine and Nanotechnology)
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26 pages, 3111 KB  
Article
Preclinical Investigation of PLGA Nanocapsules and Nanostructured Lipid Carriers for Organoselenium Delivery: Comparative In Vitro Toxicological Profile and Anticancer Insights
by Bianca Costa Maia-do-Amaral, Taís Baldissera Pieta, Luisa Fantoni Zanon, Gabriele Cogo Carneosso, Laísa Pes Nascimento, Nayra Salazar Rocha, Bruna Fracari do Nascimento, Letícia Bueno Macedo, Tielle Moraes de Almeida, Oscar Endrigo Dorneles Rodrigues, Scheila Rezende Schaffazick, Clarice Madalena Bueno Rolim and Daniele Rubert Nogueira-Librelotto
Pharmaceutics 2026, 18(1), 57; https://doi.org/10.3390/pharmaceutics18010057 - 31 Dec 2025
Viewed by 427
Abstract
Background/Objectives: Cancer is a major health concern involving abnormal cell growth. Combining anticancer agents can enhance efficacy and overcome resistance by targeting multiple pathways and creating synergistic effects. Methods: This study used in silico approaches to evaluate the physicochemical and pharmacokinetic profiles of [...] Read more.
Background/Objectives: Cancer is a major health concern involving abnormal cell growth. Combining anticancer agents can enhance efficacy and overcome resistance by targeting multiple pathways and creating synergistic effects. Methods: This study used in silico approaches to evaluate the physicochemical and pharmacokinetic profiles of the innovative organoselenium nucleoside analog Di3a, followed by the design of two nanocarriers. Di3a-loaded PLGA nanocapsules and nanostructured lipid carriers based on compritol were prepared and evaluated alone and combined with doxorubicin (DOX) and docetaxel (DTX) for a synergistic effect. Results: Di3a subtly violated some of Lipinski’s rules, but still showed suitable pharmacokinetic properties. Both nanoparticles presented nanometric size, negative zeta potential and polydispersity index values < 0.20. Hemolysis assay suggested a pH-dependent pattern conferred by the surfactant 77KL, and evidenced the biocompatibility of the formulations, aligning with the results observed in the nontumor L929 cell line. The lack of drug release studies under varying pH conditions constitutes a limitation and warrants further investigation to validate the pH-responsive properties of the nanocarriers. MTT assay revealed that both formulations exhibited significant cytotoxic effects in the A549 cell line. However, neither formulation exhibited marked toxicity toward NCI/ADR-RES, a resistant tumor cell line. Conversely, when combined with DOX or DTX, the treatments were able to sensitize these resistant cells, achieving expressive synergistic antitumor activity. Conclusions: Despite the limitations in the in silico studies, the study highlights the potential of combining the proposed nanocarriers with conventional antitumor drugs to sensitize multidrug-resistant cancer cells and emphasizes the safety of the developed nanoformulations. Full article
(This article belongs to the Special Issue Application of PLGA Nanoparticles in Cancer Therapy)
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26 pages, 1734 KB  
Review
Systems for Mitochondria-Protective Cosmetic Actives: Opportunities in Post-Oncologic Skin Regeneration
by Agata Burzyńska, Agata Wawrzyńczak and Agnieszka Feliczak-Guzik
Cosmetics 2026, 13(1), 7; https://doi.org/10.3390/cosmetics13010007 - 29 Dec 2025
Viewed by 544
Abstract
Post-oncologic skin is subject to multiple structural and functional impairments following chemotherapy and radiotherapy, including delayed epidermal turnover, compromised barrier integrity, and mitochondrial dysfunction. These changes can lead to persistent dryness, heightened reactivity, impaired regeneration, and reduced patient quality of life. In this [...] Read more.
Post-oncologic skin is subject to multiple structural and functional impairments following chemotherapy and radiotherapy, including delayed epidermal turnover, compromised barrier integrity, and mitochondrial dysfunction. These changes can lead to persistent dryness, heightened reactivity, impaired regeneration, and reduced patient quality of life. In this context, topical dermocosmetic strategies are essential not only for improving comfort and hydration, but also for supporting key cellular pathways involved in mitochondrial protection and oxidative stress reduction. Despite the promise of natural antioxidant actives, their cutaneous efficacy is often limited by poor stability, low bioavailability, and insufficient penetration of the stratum corneum. The use of nanocarriers promotes deeper skin penetration, protects oxidation-prone antioxidant compounds, and enables a controlled and prolonged release profile. This review summarizes the current evidence (2020–2025) on skin delivery systems designed to enhance the efficacy, stability, and skin penetration of antioxidants. Knowledge gaps and future directions are outlined, highlighting how rationally engineered delivery systems for mitochondria-targeted actives could contribute to safer, more effective strategies for post-oncologic skin regeneration. Full article
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47 pages, 10163 KB  
Review
Nanomedicine in Ovarian Cancer: Advances in Imaging, Targeted Delivery, and Theranostic Therapeutic Platforms
by Dorota Bartusik-Aebisher, Izabella Wilk and David Aebisher
Cancers 2026, 18(1), 86; https://doi.org/10.3390/cancers18010086 - 27 Dec 2025
Viewed by 587
Abstract
Ovarian cancer continues to be the most lethal gynaecological malignancy, principally due to its late-stage diagnosis, extensive peritoneal dissemination, chemoresistance, and limitations of current imaging and therapeutic strategies. By optimising pharmacokinetics, refining tumour-selective drug delivery, and supporting high-resolution, multimodal imaging, nanomedicine offers a [...] Read more.
Ovarian cancer continues to be the most lethal gynaecological malignancy, principally due to its late-stage diagnosis, extensive peritoneal dissemination, chemoresistance, and limitations of current imaging and therapeutic strategies. By optimising pharmacokinetics, refining tumour-selective drug delivery, and supporting high-resolution, multimodal imaging, nanomedicine offers a versatile platform to address these limitations. In this review, current progress across lipid-based, polymeric, inorganic, hybrid, and biomimetic nanocarriers is synthesised, emphasising how tailored physiochemical properties, surface functionalisation, and stimuli-responsive designs can improve tumour localisation, surmount stromal and ascetic barriers, and enable controlled drug release. Concurrently, significant advancement in imaging nanoprobes, including magnetic resonance imaging (MRI), positron emission tomography (PET)/single-photon emission computed tomography (SPECT), optical, near-infrared imaging (NIR), ultrasound, and photoacoustic systems, has evolved early lesion detection, intraoperative guidance, and quantitative monitoring of treatment. Diagnosis and therapy are further integrated within single platforms by emerging theranostic constructs, encouraging real-time visualisation of drug distribution and treatment response. Additionally, immune-nanomedicine, intraperitoneal depot systems, and nucleic acid-centred nanotherapies offer promising strategies to address immune suppression and molecular resistance in advanced ovarian cancer. In spite of noteworthy achievements, clinical translation is limited by complex manufacturing requirements, challenges with safety and stability, and restricted patient stratification. To unlock the full clinical potential of nanotechnology in ovarian cancer management, constant innovation in scalable design, regulatory standardisation, and integration of precision biomarkers will be necessary. Full article
(This article belongs to the Section Methods and Technologies Development)
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40 pages, 2651 KB  
Review
Redefining the Limits of Nanodevices-Based Drug Delivery Systems: Extracellular Vesicles
by Marina Lucia Díaz, Victoria Simón, Luciano Alejandro Benedini and Paula Verónica Messina
Pharmaceutics 2025, 17(12), 1617; https://doi.org/10.3390/pharmaceutics17121617 - 16 Dec 2025
Viewed by 577
Abstract
Extracellular vesicles (EVs) are naturally occurring cell-derived vesicles that contain the same nucleic acids, proteins, and lipids as their source cells. These nano-sized systems, which are derived from a wide range of cell types within an organism and are present in all body [...] Read more.
Extracellular vesicles (EVs) are naturally occurring cell-derived vesicles that contain the same nucleic acids, proteins, and lipids as their source cells. These nano-sized systems, which are derived from a wide range of cell types within an organism and are present in all body fluids. EVs play a crucial role both in health and disease, particularly in cancer and neurodegenerative disorders. Due to their particular structure, they can function as natural carriers for therapeutic agents and drugs, akin to synthetic liposomes. EVs exhibit numerous advantages over conventional synthetic nanocarriers and other lipid-based delivery systems, including their favorable biocompatibility, natural blood–brain barrier penetration, and capacity for gene delivery. However, EVs’ complex characterization and standardization, as well as being more expensive than other vesicular systems, are major drawbacks that need to be addressed before drug loading. The present review introduces the classification of EVs and their physiological roles, currently popular methods for isolating and purifying EVs, the main therapeutic approaches of EV-mediated drug delivery, and the functionalization of EVs as carriers. Consequently, it establishes novel pathways for advancing EV-based therapeutic methodologies across diverse medical disciplines. The study concludes with a discussion of the new challenges and future perspectives related to the clinical application of EVs. Full article
(This article belongs to the Special Issue Biomimetic Nanoparticles for Disease Treatment and Diagnosis)
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40 pages, 2992 KB  
Review
Advances in Mesoporous Silica and Hybrid Nanoparticles for Drug Delivery: Synthesis, Functionalization, and Biomedical Applications
by Ahmad Almatroudi
Pharmaceutics 2025, 17(12), 1602; https://doi.org/10.3390/pharmaceutics17121602 - 12 Dec 2025
Cited by 1 | Viewed by 880
Abstract
Mesoporous silica nanoparticles (MSNs) are among the most adaptable nanocarriers in modern pharmaceutics, characterized by a high surface area, tunable pore size, controllable morphology, and excellent biocompatibility. These qualities enable effective encapsulation, protection, and the delivery of drugs in a specific area and, [...] Read more.
Mesoporous silica nanoparticles (MSNs) are among the most adaptable nanocarriers in modern pharmaceutics, characterized by a high surface area, tunable pore size, controllable morphology, and excellent biocompatibility. These qualities enable effective encapsulation, protection, and the delivery of drugs in a specific area and, therefore, MSNs are powerful platforms for the targeted and controlled delivery of drugs and theragnostic agents. Over the past ten years and within the 2021–2025 period, the advancement of MSN design has led to the creation of hybrid nanostructures into polymers, lipids, metals, and biomolecules that have yielded multifunctional carriers with enhanced stability, responsiveness, and biological activities. The current review provides a review of the synthesis methods, surface functionalization techniques, and physicochemical characterization techniques that define the next-generation MSN-based delivery systems. The particular focus is put on stimuli-responsive systems, such as redox, pH, enzyme-activated, and light-activated systems, that enable delivering drugs in a controlled and localized manner. We further provide a summary of the biomedical use of MSNs and their hybrids such as in cancer chemotherapy, gene and nucleic acid delivery, antimicrobial and vaccine delivery, and central nervous system targeting, supported by recent in vivo and in vitro studies. Important evaluations of biocompatibility, immunogenicity, degradation, and biodistribution in vivo are also provided with a focus on safety in addition to the regulatory impediments to clinical translation. The review concludes by saying that there are still limitations such as large-scale reproducibility, long-term toxicity, and standardization by the regulators, and that directions are being taken in the future in the fields of smart programmable nanocarriers, green synthesis, and sustainable manufacture. Overall, mesoporous silica and hybrid nanoparticles represent a breakthrough technology in the nanomedicine sector with potentials that are unrivaled in relation to targeted, controlled, and personalized therapeutic interventions. Full article
(This article belongs to the Section Drug Delivery and Controlled Release)
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18 pages, 3761 KB  
Article
Hexapeptide-Liposome Nanosystem for the Delivery of Endosomal pH Modulator to Treat Acute Lung Injury
by Yuting Ji, Qian Wang, Rujing Lin, Mimi Pang, Liya Sun, Jiameng Gong, Huiqiang Ma, Shan-Yu Fung and Hong Yang
J. Funct. Biomater. 2025, 16(12), 450; https://doi.org/10.3390/jfb16120450 - 1 Dec 2025
Viewed by 731
Abstract
The overactivation of endosomal Toll-like receptor (TLR) in macrophages plays an important role in the pathogenesis of acute lung injury (ALI). There is currently still a lack of nano-formulated and macrophage-targeted endosomal TLR inhibitors that have been approved for clinical uses. We previously [...] Read more.
The overactivation of endosomal Toll-like receptor (TLR) in macrophages plays an important role in the pathogenesis of acute lung injury (ALI). There is currently still a lack of nano-formulated and macrophage-targeted endosomal TLR inhibitors that have been approved for clinical uses. We previously discovered that the elevation of endosomal pH using nanodevices provides a promising strategy to specifically inhibit endosomal TLRs in macrophages. The weakly basic drug hydroxychloroquine (HCQ) has been reported for its capability to accumulate in endolysosomes and modulate the acidity in these compartments. To enhance its macrophage-targeting ability and the therapeutic efficacy in vivo, herein we formulated HCQ into a nanoform using liposomes, named HCQ-L. We found that HCQ-L was less cytotoxic and more effective in inhibiting endosomal TLRs (including TLR3, TLR4, TLR 7/8) than the molecular HCQ. Subsequently, a hexapeptide, Pep12, was inserted onto the surface of HCQ-L to form HCQ-L-P12. Interestingly, Pep12 modification significantly improved the stability of liposomes in aqueous solution for at least 2 years; while having enhanced inhibitory effects on TLR7/8 signaling, HCQ-L-P12 displayed similar effects on inhibiting the TLR4 pathway and down-stream pro-inflammatory cytokine production when compared with HCQ-L. Furthermore, both HCQ nanoformulations potently elevated the endosomal pH. In vivo evaluation showed that HCQ-L-P12 and HCQ-L (but not molecular HCQ) were able to alleviate lung inflammation and injuries by decreasing inflammatory cell infiltration upon intratracheal instillation in a lipopolysaccharide (LPS)-induced acute lung injury (ALI) mouse model. This research provides a new strategy to fabricate lipid-based nanocarriers for targeted delivery of endosomal pH modulators to treat ALI and other acute and chronic inflammatory disorders. Full article
(This article belongs to the Special Issue Nanomaterials for Drug Delivery Systems)
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26 pages, 2505 KB  
Review
Advancements in Nanotheranostic Approaches for Tuberculosis: Bridging Diagnosis, Prevention, and Therapy Through Smart Nanoparticles
by Renée Onnainty and Gladys E. Granero
J. Nanotheranostics 2025, 6(4), 33; https://doi.org/10.3390/jnt6040033 - 1 Dec 2025
Viewed by 610
Abstract
Tuberculosis (TB), caused by Mycobacterium tuberculosis, continues to be a leading cause of death from a single infectious agent worldwide. Conventional antibiotic therapies face significant limitations, including multidrug resistance, poor treatment adherence, limited penetration into granulomas, and systemic toxicity. Recent advances in [...] Read more.
Tuberculosis (TB), caused by Mycobacterium tuberculosis, continues to be a leading cause of death from a single infectious agent worldwide. Conventional antibiotic therapies face significant limitations, including multidrug resistance, poor treatment adherence, limited penetration into granulomas, and systemic toxicity. Recent advances in nanomedicine have paved the way for nanotheranostic approaches that integrate therapeutic, diagnostic, and preventive functions into a single platform. Nanotheranostic systems enable targeted drug delivery to infected macrophages and granulomatous lesions, real-time imaging for disease monitoring, and controlled, stimuli-responsive release of antitubercular agents. These platforms can be engineered to modulate host immune responses through host-directed therapies (HDTs), including the induction of autophagy, regulation of apoptosis, and macrophage polarization toward the bactericidal M1 phenotype. Additionally, nanocarriers can co-deliver antibiotics, immunomodulators, or photosensitizers to enhance intracellular bacterial clearance while minimizing off-target toxicity. The review also discusses the potential of nanotechnology to improve TB prevention by enhancing vaccine efficacy, stability, and targeted delivery of immunogens such as BCG and novel subunit vaccines. Key nanoplatforms, including polymeric, lipid-based, metallic, and hybrid nanoparticles, are highlighted, along with design principles for optimizing biocompatibility, multifunctionality, and clinical translatability. Collectively, nanotheranostic strategies represent a transformative approach to TB management, bridging diagnosis, therapy, and prevention in a single, adaptable platform to address the unmet needs of this global health challenge. Full article
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20 pages, 1053 KB  
Systematic Review
Advancing Photodynamic Cancer Therapy with Smart Light-Responsive Lipid and Polymeric Nanocarriers: Evidence from a Meta-Analysis of Efficacy and Pharmacokinetics
by Ahmed M. Agiba, Rabab A. El-Gazar, Mohamed A. Mekkawy, Nihal Elsayyad, Hala N. ElShagea, Patricia Segura-Medina and Raghda Rabe Hamed
Pharmaceuticals 2025, 18(12), 1796; https://doi.org/10.3390/ph18121796 - 25 Nov 2025
Viewed by 509
Abstract
Background/Objectives: Conventional anticancer drugs often exhibit limited solubility and bioavailability due to unfavorable physicochemical properties and inherent physiological barriers. To overcome these persistent challenges, nanocarriers have been developed to enhance drug bioavailability and therapeutic efficacy. Among these, lipid and polymeric nanocarriers (LP-NCs) [...] Read more.
Background/Objectives: Conventional anticancer drugs often exhibit limited solubility and bioavailability due to unfavorable physicochemical properties and inherent physiological barriers. To overcome these persistent challenges, nanocarriers have been developed to enhance drug bioavailability and therapeutic efficacy. Among these, lipid and polymeric nanocarriers (LP-NCs) have emerged as particularly promising candidates for anticancer drug delivery. These systems can be engineered for targeted delivery and tailored to respond to specific stimuli, thereby enhancing their therapeutic potential. A notable advancement in this field is the development of smart light-responsive LP-NCs, which demonstrate superior performance over conventional nanocarriers by enabling controlled drug release in response to external light stimuli. Methods: This study presents a meta-analysis based on a curated selection of publications from multiple scientific databases and literature sources. The objective was to evaluate whether light-responsive LP-NCs offer superior anticancer drug bioavailability and therapeutic efficacy compared with their conventional counterparts. The primary outcome measure was the pharmacokinetic parameter area under the curve (AUC), derived from in vivo animal studies. Results: The analysis revealed a significant increase in AUC for light-responsive LP-NCs, indicating improved drug bioavailability and prolonged systemic exposure. Conclusions: These findings highlight the potential of LP-NCs as a promising strategy for enhancing targeted anticancer drug delivery. This approach could pave the way for more effective therapeutic interventions and warrants further investigation in future research and clinical trials. Full article
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41 pages, 2193 KB  
Review
Advances in Lipid-Polymer Hybrid Nanoparticles: Design Strategies, Functionalization, Oncological and Non-Oncological Clinical Prospects
by Shery Jacob, Namitha Raichel Varkey, Sai H. S. Boddu, Bapi Gorain, Rekha Rao and Anroop B. Nair
Pharmaceuticals 2025, 18(12), 1772; https://doi.org/10.3390/ph18121772 - 21 Nov 2025
Cited by 1 | Viewed by 2494
Abstract
Lipid-polymer hybrid nanoparticles (LPHNPs) are the next-generation nanocarriers that integrate the mechanical strength and sustained-release capacity of polymeric cores with the biocompatibility and high drug-loading efficiency of lipid shells. Various design strategies and architectures that enhance encapsulation efficiency, stability, and targeted delivery of [...] Read more.
Lipid-polymer hybrid nanoparticles (LPHNPs) are the next-generation nanocarriers that integrate the mechanical strength and sustained-release capacity of polymeric cores with the biocompatibility and high drug-loading efficiency of lipid shells. Various design strategies and architectures that enhance encapsulation efficiency, stability, and targeted delivery of diverse therapeutic agents are reviewed. Commonly employed polymers, lipids, and surfactants that enable controlled drug release and enhanced pharmacokinetic performance are summarized in tabular form, while fabrication methods such as single-step, emulsification-solvent evaporation, and microfluidic techniques are discussed for their scalability and reproducibility. The therapeutic potential of LPHNPs in delivering poorly soluble drugs, phytochemicals, and genetic materials achieving synergistic therapeutic outcomes in oncological applications is comprehensively highlighted. The manuscript also includes details on ligand-based functionalization and the integration of imaging and stimuli-responsive elements to enhance targeted delivery and develop multifunctional theranostic LPHNPs systems. Furthermore, non-oncologic applications of LPHNPs in ocular, topical, and oral delivery are discussed, emphasizing their potential in treating inflammatory, infectious, and autoimmune disorders with sustained release and enhanced therapeutic efficacy. Recent patents focusing on improved biocompatibility, dual-drug encapsulation, and mRNA delivery are summarized. However, challenges such as large-scale production, reproducibility, safety, and regulatory standardization must be addressed through quality by design approaches and advanced manufacturing technologies to fully realize the clinical and commercial potential of next-generation LPHNPs. Full article
(This article belongs to the Section Pharmaceutical Technology)
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37 pages, 7790 KB  
Review
Cyclodextrin: Dual Functions as a Therapeutic Agent and Nanocarrier for Regulating Cholesterol Homeostasis in Atherosclerosis
by Hao Cui, Yaqi Xu, Shulin Pu, Xue Guo, Danyu Zhao, Yuan Liu, Ye Yang and Chengxiao Wang
Pharmaceutics 2025, 17(11), 1496; https://doi.org/10.3390/pharmaceutics17111496 - 19 Nov 2025
Viewed by 1124
Abstract
The progression of atherosclerosis (AS) is strongly linked to lipid crystals accumulation caused by cholesterol metabolism disorders and the worsening of the inflammatory microenvironment. Cyclodextrin (CD), characterized by their unique hydrophobic cavity structure, effectively solubilize cholesterol crystals (CCs) through host–guest recognition and act [...] Read more.
The progression of atherosclerosis (AS) is strongly linked to lipid crystals accumulation caused by cholesterol metabolism disorders and the worsening of the inflammatory microenvironment. Cyclodextrin (CD), characterized by their unique hydrophobic cavity structure, effectively solubilize cholesterol crystals (CCs) through host–guest recognition and act as a multifunctional nanocarrier core, facilitating synergistic therapy that combines pharmaceutical and adjuvant properties. CD-based nano drug delivery systems (CD-NDDS) enable precise targeting of atherosclerotic plaques. By employing synergistic functions (e.g., CCs solubilization, cholesterol efflux promotion via ABCA1/ABCG1 pathways, inflammasome inhibition, and inflammatory microenvironment alleviation), this system provides an effective strategy for AS therapy. Furthermore, CD-NDDS bestows additional pharmaceutical attributes, including enhanced solubility, controlled release, and responsive stimulation. This review begins by elucidating the intrinsic relationship between cholesterol and AS, followed by an examination of the structure-activity relationship governing CD’s cholesterol adsorption. It then explores the construction strategies, structural characteristics, and targeting mechanisms of CD nanodelivery systems in detail. The work systematically assesses CD’s formulation and pharmacological properties in targeted nanodelivery systems for combating AS, integrating drugs and adjuvants. Finally, future research directions are outlined, addressing biocompatibility optimization, targeting efficiency enhancement, and clinical translation challenges to provide a theoretical foundation and technical guidance for precise AS treatment. Full article
(This article belongs to the Special Issue Recent Advances in Nanotechnology Therapeutics)
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32 pages, 2730 KB  
Review
Imatinib in Targeted Therapy: Advances in Biomedical Applications and Drug Delivery Systems
by Yana Gvozdeva, Petya Georgieva and Plamen Katsarov
Hemato 2025, 6(4), 40; https://doi.org/10.3390/hemato6040040 - 12 Nov 2025
Viewed by 1833
Abstract
Imatinib (IMT) is a small-molecule tyrosine kinase inhibitor that primarily targets platelet-derived growth factor receptor-β and related kinases. Beyond its established efficacy in chronic myeloid leukemia, IMT has also demonstrated therapeutic benefits in gastrointestinal stromal tumors, dermatofibrosarcoma, acute lymphoblastic leukemia, and as a [...] Read more.
Imatinib (IMT) is a small-molecule tyrosine kinase inhibitor that primarily targets platelet-derived growth factor receptor-β and related kinases. Beyond its established efficacy in chronic myeloid leukemia, IMT has also demonstrated therapeutic benefits in gastrointestinal stromal tumors, dermatofibrosarcoma, acute lymphoblastic leukemia, and as a second-line treatment for aggressive systemic mastocytosis or as an anti-Mycobacterium agent. From a physicochemical perspective, IMT exhibits poor aqueous solubility but high membrane permeability, classifying it as a Biopharmaceutics Classification System Class II compound. Pharmacokinetically, IMT shows variable oral absorption and a prolonged terminal half-life, resulting in dose-dependent systemic exposure. Despite relatively high oral bioavailability, its clinical use requires large doses to achieve therapeutic efficacy, underscoring the need for advanced drug delivery strategies. Nano- and microscale delivery systems offer promising approaches to enhance tumor-specific accumulation through the enhanced permeability and retention effect while mitigating resistance mechanisms. However, achieving high drug loading introduces formulation challenges, such as controlling particle size distribution, polydispersity, and scalability. Moreover, designing carriers capable of controlled release without premature leakage remains crucial for maintaining systemic bioavailability and therapeutic performance. Emerging delivery platforms—including polymeric, lipid-based, carbon-derived, and stimuli-responsive nanocarriers—have shown significant potential in overcoming these limitations. Such systems can enhance IMT’s bioavailability, improve selective tumor targeting, and minimize systemic toxicity, thereby advancing its translational potential. This review aims to highlight the different biomedical applications of IMT and off-label uses, and to discuss current advances in drug delivery to optimize its clinical efficacy and safety profile. Full article
(This article belongs to the Section Chronic Myeloid Disease)
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