Sign in to use this feature.

Years

Between: -

Subjects

remove_circle_outline
remove_circle_outline
remove_circle_outline
remove_circle_outline
remove_circle_outline
remove_circle_outline
remove_circle_outline
remove_circle_outline
remove_circle_outline

Journals

remove_circle_outline
remove_circle_outline
remove_circle_outline
remove_circle_outline
remove_circle_outline
remove_circle_outline
remove_circle_outline

Article Types

Countries / Regions

remove_circle_outline
remove_circle_outline
remove_circle_outline
remove_circle_outline
remove_circle_outline

Search Results (569)

Search Parameters:
Keywords = solid-lipid nanoparticles

Order results
Result details
Results per page
Select all
Export citation of selected articles as:
29 pages, 2060 KiB  
Review
Revitalizing Colchicine: Novel Delivery Platforms and Derivatives to Expand Its Therapeutic Potential
by Natallia V. Dubashynskaya, Anton N. Bokatyi, Mikhail M. Galagudza and Yury A. Skorik
Int. J. Mol. Sci. 2025, 26(15), 7591; https://doi.org/10.3390/ijms26157591 - 6 Aug 2025
Abstract
Colchicine is a potent alkaloid with well-established anti-inflammatory properties. It shows significant promise in treating classic immune-mediated inflammatory diseases, as well as associated cardiovascular diseases, including atherosclerosis. However, its clinical use is limited by a narrow therapeutic window, dose-limiting systemic toxicity, variable bioavailability, [...] Read more.
Colchicine is a potent alkaloid with well-established anti-inflammatory properties. It shows significant promise in treating classic immune-mediated inflammatory diseases, as well as associated cardiovascular diseases, including atherosclerosis. However, its clinical use is limited by a narrow therapeutic window, dose-limiting systemic toxicity, variable bioavailability, and clinically significant drug–drug interactions, partly mediated by modulation of P-glycoprotein and cytochrome P450 3A4 metabolism. This review explores advanced delivery strategies designed to overcome these limitations. We critically evaluate lipid-based systems, such as solid lipid nanoparticles, liposomes, transferosomes, ethosomes, and cubosomes; polymer-based nanoparticles; microneedles; and implants, including drug-eluting stents. These systems ensure targeted delivery, improve pharmacokinetics, and reduce toxicity. Additionally, we discuss chemical derivatization approaches, such as prodrugs, codrugs, and strategic ring modifications (A-, B-, and C-rings), aimed at optimizing both the efficacy and safety profile of colchicine. Combinatorial nanoformulations that enable the co-delivery of colchicine with synergistic agents, such as glucocorticoids and statins, as well as theranostic platforms that integrate therapeutic and diagnostic functions, are also considered. These innovative delivery systems and derivatives have the potential to transform colchicine therapy by broadening its clinical applications while minimizing adverse effects. Future challenges include scalable manufacturing, long-term safety validation, and the translation of research into clinical practice. Full article
(This article belongs to the Section Macromolecules)
Show Figures

Figure 1

35 pages, 1395 KiB  
Review
Local Chemotherapy of Skin Pre-Neoplastic Lesions and Malignancies from the Perspective of Current Pharmaceutics
by Nadezhda Ivanova
Pharmaceutics 2025, 17(8), 1009; https://doi.org/10.3390/pharmaceutics17081009 - 1 Aug 2025
Viewed by 470
Abstract
In the preceding and early stages of cancer progression, local drug delivery to pre-cancerous and cancerous skin lesions may be applied as an alternative or supplementary therapy. At present, 5-Fluorouracil, imiquimod, and tirbanibulin creams and ointments have established their place in practice, while [...] Read more.
In the preceding and early stages of cancer progression, local drug delivery to pre-cancerous and cancerous skin lesions may be applied as an alternative or supplementary therapy. At present, 5-Fluorouracil, imiquimod, and tirbanibulin creams and ointments have established their place in practice, while several other active pharmaceutical ingredients (APIs) (e.g., calcipotriol, tretinoin, diclofenac) have been repurposed, used off-label, or are currently being investigated in mono- or combined chemotherapies of skin cancers. Apart from them, dozens to hundreds of therapeutics of natural and synthetic origin are proven to possess anti-tumor activity against melanoma, squamous cell carcinoma (SCC), and other skin cancer types in in vitro studies. Their clinical introduction is most often limited by low skin permeability, challenged targeted drug delivery, insufficient chemical stability, non-selective cytotoxicity, or insufficient safety data. A variety of prodrug and nanotechnological approaches, including vesicular systems, micro- and nanoemulsions, solid lipid nanoparticles, nanostructured lipid carriers, polymeric nanoparticles, and others, offer versatile solutions for overcoming the biophysical barrier function of the skin and the undesirable physicochemical nature of some drug molecules. This review aims to present the most significant aspects and latest achievements on the subject. Full article
Show Figures

Figure 1

53 pages, 3300 KiB  
Review
A Comprehensive Review of Smart Thermosensitive Nanocarriers for Precision Cancer Therapy
by Atena Yaramiri, Rand Abo Asalh, Majd Abo Asalh, Nour AlSawaftah, Waad H. Abuwatfa and Ghaleb A. Husseini
Int. J. Mol. Sci. 2025, 26(15), 7322; https://doi.org/10.3390/ijms26157322 - 29 Jul 2025
Viewed by 441
Abstract
By 2030, millions of new cancer cases will be diagnosed, as well as millions of cancer-related deaths. Traditional drug delivery methods have limitations, so developing smart drug delivery systems (SDDs) has emerged as a promising avenue for more effective and precise cancer treatment. [...] Read more.
By 2030, millions of new cancer cases will be diagnosed, as well as millions of cancer-related deaths. Traditional drug delivery methods have limitations, so developing smart drug delivery systems (SDDs) has emerged as a promising avenue for more effective and precise cancer treatment. Nanotechnology, particularly nanomedicine, provides innovative approaches to enhance drug delivery, including the use of nanoparticles. One such type of SDD is thermosensitive nanoparticles, which respond to internal and external stimuli, such as temperature changes, to release drugs precisely at tumor sites and minimize off-target effects. On the other hand, hyperthermia is a cancer treatment mode that goes back centuries and has become popular because it can target cancer cells while sparing healthy tissue. This paper presents a comprehensive review of smart thermosensitive nanoparticles for cancer treatment, with a primary focus on organic nanoparticles. The integration of hyperthermia with temperature-sensitive nanocarriers, such as micelles, hydrogels, dendrimers, liposomes, and solid lipid nanoparticles, offers a promising approach to improving the precision and efficacy of cancer therapy. By leveraging temperature as a controlled drug release mechanism, this review highlights the potential of these innovative systems to enhance treatment outcomes while minimizing adverse side effects. Full article
(This article belongs to the Section Molecular Oncology)
Show Figures

Figure 1

43 pages, 3721 KiB  
Review
Novel Strategies for the Formulation of Poorly Water-Soluble Drug Substances by Different Physical Modification Strategies with a Focus on Peroral Applications
by Julian Quodbach, Eduard Preis, Frank Karkossa, Judith Winck, Jan Henrik Finke and Denise Steiner
Pharmaceuticals 2025, 18(8), 1089; https://doi.org/10.3390/ph18081089 - 23 Jul 2025
Viewed by 803
Abstract
The number of newly developed substances with poor water solubility continually increases. Therefore, specialized formulation strategies are required to overcome the low bioavailability often associated with this property. This review provides an overview of novel physical modification strategies discussed in the literature over [...] Read more.
The number of newly developed substances with poor water solubility continually increases. Therefore, specialized formulation strategies are required to overcome the low bioavailability often associated with this property. This review provides an overview of novel physical modification strategies discussed in the literature over the past decades and focuses on oral dosage forms. A distinction is made between ‘brick-dust’ molecules, which are characterized by high melting points due to the solid-state properties of the substances, and ‘grease-ball’ molecules with high lipophilicity. In general, the discussed strategies are divided into the following three main categories: drug nanoparticles, solid dispersions, and lipid-based formulations. Full article
(This article belongs to the Collection Feature Review Collection in Pharmaceutical Technology)
Show Figures

Graphical abstract

39 pages, 1536 KiB  
Review
Transdermal Drug Delivery Systems: Methods for Enhancing Skin Permeability and Their Evaluation
by Elena O. Bakhrushina, Marina M. Shumkova, Yana V. Avdonina, Arsen A. Ananian, Mina Babazadeh, Ghazaleh Pouya, Viktoria V. Grikh, Irina M. Zubareva, Svetlana I. Kosenkova, Ivan I. Krasnyuk and Ivan I. Krasnyuk
Pharmaceutics 2025, 17(7), 936; https://doi.org/10.3390/pharmaceutics17070936 - 20 Jul 2025
Viewed by 927
Abstract
Transdermal drug delivery (TDD) is an increasingly important non-invasive method for administering active pharmaceutical ingredients (APIs) through the skin barrier, offering advantages such as improved therapeutic efficacy and reduced systemic side effects. As demand increases for patient-friendly and minimally invasive treatment options, TDD [...] Read more.
Transdermal drug delivery (TDD) is an increasingly important non-invasive method for administering active pharmaceutical ingredients (APIs) through the skin barrier, offering advantages such as improved therapeutic efficacy and reduced systemic side effects. As demand increases for patient-friendly and minimally invasive treatment options, TDD has attracted substantial attention in research and clinical practice. This review summarizes recent advances enhancing skin permeability through chemical enhancers (e.g., ethanol, fatty acids, terpenes), physical (e.g., iontophoresis, microneedles, sonophoresis), and nanotechnological methods (e.g., liposomes, ethosomes, solid lipid nanoparticles, and transferosomes). A comprehensive literature analysis, including scientific publications, regulatory guidelines, and patents, was conducted to identify innovative methods and materials used to overcome the barrier properties of the stratum corneum. Special emphasis was placed on in vitro, ex vivo, and in vivo evaluation techniques for such as Franz diffusion cells for assessing drug permeation and skin interactions. The findings highlight the importance of active physical methods, passive nanostructured systems, and chemical penetration enhancers. In conclusion, integrating multiple analytical techniques is essential for the rational design and optimization of effective transdermal drug delivery systems. Full article
(This article belongs to the Special Issue Dermal and Transdermal Drug Delivery Systems)
Show Figures

Graphical abstract

26 pages, 808 KiB  
Review
A Review of Formulation Strategies for Cyclodextrin-Enhanced Solid Lipid Nanoparticles (SLNs) and Nanostructured Lipid Carriers (NLCs)
by Tarek Alloush and Burcu Demiralp
Int. J. Mol. Sci. 2025, 26(13), 6509; https://doi.org/10.3390/ijms26136509 - 6 Jul 2025
Viewed by 962
Abstract
The advancement of efficient drug delivery systems continues to pose a significant problem in pharmaceutical sciences, especially for compounds with limited water solubility. Lipid-based systems, including solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs), have emerged as viable options owing to their [...] Read more.
The advancement of efficient drug delivery systems continues to pose a significant problem in pharmaceutical sciences, especially for compounds with limited water solubility. Lipid-based systems, including solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs), have emerged as viable options owing to their biocompatibility, capability to safeguard labile chemicals, and potential for prolonged release. Nonetheless, the encapsulation efficiency (EE) and release dynamics of these carriers can be enhanced by including cyclodextrins (CDs)—cyclic oligosaccharides recognized for their ability to form inclusion complexes with hydrophobic compounds. This article offers an extensive analysis of CD-modified SLNs and NLCs as multifunctional drug delivery systems. The article analyses the fundamental principles of these systems, highlighting the pre-complexation of the drug with cyclodextrins before lipid incorporation, co-encapsulation techniques, and surface adsorption after formulation. Attention is concentrated on the physicochemical interactions between cyclodextrins and lipid matrices, which influence essential factors such as particle size, encapsulation efficiency, and colloidal stability. The review includes characterization techniques, such as particle size analysis, zeta potential measurement, drug release studies, and Fourier-transform infrared spectroscopy (FT-IR)/Nuclear Magnetic Resonance (NMR) analyses. The study highlights the application of these systems across many routes of administration, including oral, topical, and mucosal, illustrating their adaptability and potential for targeted delivery. The review outlines current formulation challenges, including stability issues, drug leakage, and scalability concerns, and proposes solutions through advanced approaches, such as stimuli-responsive release mechanisms and computer modeling for system optimization. The study emphasizes the importance of regulatory aspects and outlines future directions in the development of CD-lipid hybrid nanocarriers, showcasing its potential to revolutionize the delivery of poorly soluble drugs. Full article
(This article belongs to the Special Issue Research on Cyclodextrin)
Show Figures

Graphical abstract

22 pages, 7596 KiB  
Article
Optimization of Solid Lipid Nanoparticle Formulation Using Design of Experiments, PART I: Strategic Tool for the Determination of Critical Parameters Regarding Formulation and Process
by Margot Cassayre, Dany Teles de Souza, Magalie Claeys-Bruno, Alexandre Altié, Philippe Piccerelle and Christophe Sauzet
Nanomaterials 2025, 15(13), 1034; https://doi.org/10.3390/nano15131034 - 3 Jul 2025
Viewed by 468
Abstract
This study presents a methodological framework for optimizing “blank” solid lipid nanoparticles (SLNs), focusing on the use of a design of experiments (DOE) approach. Rather than emphasizing the applications of SLNs, the objective is to identify and optimize critical formulation and process parameters—specifically [...] Read more.
This study presents a methodological framework for optimizing “blank” solid lipid nanoparticles (SLNs), focusing on the use of a design of experiments (DOE) approach. Rather than emphasizing the applications of SLNs, the objective is to identify and optimize critical formulation and process parameters—specifically those influencing particle size (PS), polydispersity index (PDI), and zeta potential (ZP)—during early development stages. A non-classical mixed design was applied using AZURAD® software (version 4.4.1), incorporating a mixture variable for lipid composition (comprising carnauba wax, glyceryl behenate, glyceryl distearate), and two quantitative factors: the percentage of polysorbate 80 (P80) in the P80/sorbitan oleate surfactant system and ultrasound (US) treatment time. The DOE analysis identified P80 concentration as a key parameter, with optimal formulations observed when P80 ranged between 35% and 45%. A fixed P80 ratio of 41% and a US time of 7.5 min enabled precise adjustment of lipid composition. Following a desirability function analysis, an optimized formulation was obtained with a PS of 176.3 ± 2.78 nm, a PDI of 0.268 ± 0.022, and a ZP of −35.5 ± 0.36 mV. These findings validate the relevance of our DOE-based strategy, offering a scalable, cost-effective platform that reduces material use, time, and analytical effort in SLN development. Full article
(This article belongs to the Special Issue Modeling, Simulation and Optimization of Nanomaterials)
Show Figures

Figure 1

19 pages, 3764 KiB  
Article
Isolation and Characterization of Tissue-Derived Extracellular Vesicles from Mouse Lymph Nodes
by Bernadett R. Bodnár, Sayam Ghosal, Brachyahu M. Kestecher, Panna Királyhidi, András Försönits, Nóra Fekete, Edina Bugyik, Zsolt I. Komlósi, Éva Pállinger, György Nagy, Edit I. Buzás and Xabier Osteikoetxea
Int. J. Mol. Sci. 2025, 26(13), 6092; https://doi.org/10.3390/ijms26136092 - 25 Jun 2025
Viewed by 1783
Abstract
Extracellular vesicles (EVs) are lipid membrane-enclosed particles released by all cells and can be isolated from various sources, even from solid tissues. This study focuses on isolating and characterizing EVs from mouse lymph nodes (LNs). Male C57BL/6 mice were injected with complete Freund’s [...] Read more.
Extracellular vesicles (EVs) are lipid membrane-enclosed particles released by all cells and can be isolated from various sources, even from solid tissues. This study focuses on isolating and characterizing EVs from mouse lymph nodes (LNs). Male C57BL/6 mice were injected with complete Freund’s adjuvant, with or without ovalbumin. Inguinal and popliteal LNs were incised 9 days after immunization, and EV isolation was carried out using a combination of differential centrifugation and size-exclusion chromatography. The characteristic morphology of small and large EVs was confirmed by transmission electron microscopy. Particle size distribution and concentration were determined by nanoparticle tracking analysis, while protein and lipid contents were measured by bicinchoninic acid assay, and sulfo-phospho-vanillin assays, respectively, to calculate the protein-to-lipid ratio. Immune and EV markers were analyzed by using flow cytometry and Western blot assay, revealing significant changes between immunized mice compared to controls. This study establishes a novel protocol for isolating and characterizing EVs from LNs and highlights the impact of immunization on EV properties, offering insights into their roles in immune processes. Full article
(This article belongs to the Special Issue Molecular Mechanism of Extracellular Vesicles in Human Diseases)
Show Figures

Graphical abstract

30 pages, 3428 KiB  
Review
Lipid-Polymer Hybrid Nanoparticles as a Smart Drug Delivery System for Peptide/Protein Delivery
by Alharith A. A. Hassan, Eslam Ramadan, Katalin Kristó, Géza Regdon and Tamás Sovány
Pharmaceutics 2025, 17(6), 797; https://doi.org/10.3390/pharmaceutics17060797 - 19 Jun 2025
Viewed by 1505
Abstract
The efficient oral delivery of therapeutic proteins and peptides poses a tremendous challenge due to their inherent instability, large molecular size, and susceptibility to enzymatic degradation. Several nanocarrier systems, such as liposomes, solid lipid nanoparticles, and polymeric nanoparticles, have been explored to overcome [...] Read more.
The efficient oral delivery of therapeutic proteins and peptides poses a tremendous challenge due to their inherent instability, large molecular size, and susceptibility to enzymatic degradation. Several nanocarrier systems, such as liposomes, solid lipid nanoparticles, and polymeric nanoparticles, have been explored to overcome these problems. Liposomes and other lipid-based nanocarriers show excellent biocompatibility and the ability to encapsulate hydrophobic and hydrophilic drugs; however, they often suffer from poor structural stability, premature leakage of the loaded drugs, and poor encapsulation efficiency for macromolecular peptides and proteins. On the other hand, polymeric nanoparticles are more stable and allow better control over drug release; nevertheless, they usually lack the necessary biocompatibility and cellular uptake efficiency. Recently, lipid-polymer hybrid nanoparticles (LPHNs) have emerged as an advanced solution combining the structural stability of polymers and the biocompatibility and surface functionalities of lipids to enhance the controlled release, stability, and bioavailability of protein and peptide drugs. In this review, an attempt was made to set a clear definition of the LPHNs and extend the concept and area, so to our knowledge, this is the first review that highlights six categories of the LPHNs based on their anatomy. Moreover, this review offers a detailed analysis of LPHN preparation methods, including conventional and nonconventional one-step and two-step processes, nanoprecipitation, microfluidic mixing, and emulsification methods. Moreover, the material attributes and critical process parameters affecting the output of the preparation methods were illustrated with supporting examples to enable researchers to select the suitable preparation method, excipients, and parameters to be manipulated to get the LPHNs with the predetermined quality. The number of reviews focusing on the formulation of peptide/protein pharmaceutics usually focus on a specific drug like insulin. To our knowledge, this is the first review that generally discusses LPHN-based delivery of biopharmaceuticals. by discussing representative examples of previous reports comparing them to a variety of nanocarrier systems to show the potentiality of the LPHNs to deliver peptides and proteins. Moreover, some ideas and suggestions were proposed by the authors to tackle some of the shortcomings highlighted in these studies. By presenting this comprehensive overview of LPHN preparation strategies and critically analyzing literature studies on this topic and pointing out their strong and weak points, this review has shown the gaps and enlightened avenues for future research. Full article
Show Figures

Graphical abstract

20 pages, 1824 KiB  
Article
The Impact of Essential Oils Derived from Citrus Species to Control Botrytis cinerea and Their Potential Physiological Actions
by Sebastián Campos, Javier Espinoza, Juan Mauricio Fuentes, Ignacio Jofré-Fernández, Gonzalo Tortella, Diego Navarro, Andrés Quiroz, María Cristina Diez, Olga Rubilar and Paola Fincheira
Plants 2025, 14(12), 1859; https://doi.org/10.3390/plants14121859 - 17 Jun 2025
Viewed by 811
Abstract
Botrytis cinerea is one of the phytopathogenic fungi of the greatest economic importance worldwide. Essential oils (EOs) have been proposed as a sustainable alternative to reduce the growth of phytopathogenic fungi. Nevertheless, few studies exist about its mechanisms of action. This study evaluated [...] Read more.
Botrytis cinerea is one of the phytopathogenic fungi of the greatest economic importance worldwide. Essential oils (EOs) have been proposed as a sustainable alternative to reduce the growth of phytopathogenic fungi. Nevertheless, few studies exist about its mechanisms of action. This study evaluated the antifungal activity of EOs from Citrus reticulata, Citrus limon, Citrus sinensis, and Citrus paradisi peels and their encapsulation inside solid lipid nanoparticles (SLNs). Accordingly, Citrus EOs were mainly constituted by monoterpene hydrocarbons, where limonene was the most abundant in all EOs. C. reticulata and C. limon EOs reduced the mycelial growth at above 54% after 96 h. The other EOs did not significantly impact the phytopathogen. C. reticulata EO increased the hyphae damage by 40%, but the spore germination was reduced by only 8.34%. It also significantly increased the pH, the electrical conductivity, and the release of intracellular absorbing material and soluble proteins in B. cinerea cultures. Contrary, the esterase, mitochondrial, and succinate dehydrogenase activities decreased at above 50%. C. reticulata EO into SLN reduced the mycelial growth of B. cinerea by 90–97%. These results show that the EO of C. reticulata alters the physiological and metabolic activities of B. cinerea to reduce its growth. Full article
(This article belongs to the Special Issue Nanomaterials in Plant Growth and Stress Adaptation—2nd Edition)
Show Figures

Figure 1

31 pages, 12094 KiB  
Article
Engineering Lipid–Polymer Nanoparticles for siRNA Delivery to Cancer Cells
by Arthur Manda, Abdulelah Alhazza, Hasan Uludağ and Hamidreza Montazeri Aliabadi
Pharmaceuticals 2025, 18(6), 864; https://doi.org/10.3390/ph18060864 - 10 Jun 2025
Viewed by 910
Abstract
Background: RNA interference (RNAi) is a powerful tool that can target many proteins without the expensive and time-consuming drug development studies. However, due to the challenges in delivering RNA molecules, the potential impact of RNAi approaches is yet to be fully realized [...] Read more.
Background: RNA interference (RNAi) is a powerful tool that can target many proteins without the expensive and time-consuming drug development studies. However, due to the challenges in delivering RNA molecules, the potential impact of RNAi approaches is yet to be fully realized in clinical settings. Lipid nanoparticles (LNPs) have been the most successful delivery system for nucleic acids, but targeted delivery to a solid tumor still eludes the developed LNPs. We hypothesized that specially designed low-molecular-weight PEIs can partially or completely replace the ionizable lipids for more accommodating vehicles due to the structural flexibility offered by polymers, which could lead to safer and more efficient nucleic acid delivery. Methods: To achieve this, we first optimized the LNP formulations as a point of reference for three outcomes: cellular uptake, cytotoxicity, and silencing efficiency. Using a response surface methodology (Design Expert), we optimized siRNA delivery by varying mole fractions of lipid components. Leveraging the optimal LNP formulation, we integrated specifically designed cationic polymers as partial or complete replacements for the ionizable lipid. This methodological approach, incorporating optimal combined designs and response surface methodologies, refined the LPNPs to an optimal efficiency. Results: Our data revealed that DOPE and Dlin-MC3-DMA contributed to higher efficiency in selected breast cancer cells over DSPC and ALC-0315 as neutral and ionizable lipids, respectively, based on the software analysis and direct comparative experiments. Incorporation of selected polymers enhanced the cellular internalization significantly, which in some formulations resulted in higher efficiency. Conclusions: These findings offer a framework for the rational design of LPNPs, that could enhance the passive targeting and silencing efficiency in cancer treatment and broader applications for RNAi-based strategies. Full article
Show Figures

Graphical abstract

17 pages, 8350 KiB  
Article
Characterisation and In Vitro Drug Release Profiles of Oleanolic Acid- and Asiatic Acid-Loaded Solid Lipid Nanoparticles (SLNs) for Oral Administration
by Michael Oboh, Eman Elhassan, Neil Anthony Koorbanally, Laurencia Govender, Muthulisi Siwela, Thirumala Govender and Blessing Nkazimulo Mkhwanazi
Pharmaceutics 2025, 17(6), 723; https://doi.org/10.3390/pharmaceutics17060723 - 30 May 2025
Viewed by 1585
Abstract
Objectives: This study characterised and evaluated the stability, solubility, and in vitro drug release of OA- and AA-loaded SLNs. Methods: The OA- and AA-SLNs were formulated using the emulsion solvent evaporation method and characterised based on particle size (PS), polydispersity index (PDI), zeta [...] Read more.
Objectives: This study characterised and evaluated the stability, solubility, and in vitro drug release of OA- and AA-loaded SLNs. Methods: The OA- and AA-SLNs were formulated using the emulsion solvent evaporation method and characterised based on particle size (PS), polydispersity index (PDI), zeta potential (ZP), and transmission electron microscopy (TEM). Solubility studies were conducted in PBS (pH 1.2 and 6.8) and dH2O using HPLC, while in vitro drug release was assessed in simulated intestinal fluid (SIF) (pH 6.8). Results: The optimised OA-SLNs (1:1 drug-to-lipid ratio) showed PS, PDI, ZP, and EE% values of 312.9 ± 3.617 nm, 0.157 ± 0.014, −17.0 ± 0.513 mV, and 86.54 ± 1.818%, respectively. The optimised AA-SLNs (1:2 drug-to-lipid: ratio) had a PS of 115.5 ± 0.458 nm, PDI of 0.255 ± 0.007, ZP of −11.9 ± 0.321 mV, and EE% of 76.22 ± 0.436%. The SLNs remained stable for 60 days at 4 °C and room temperature (p < 0.05). The solubility study revealed that free OA and AA showed no measurable values in the three solvents. However, OA-SLNs showed the highest solubility in H2O (16-fold) followed by PBS at pH 6.8 (10-fold) and pH 1.2 (10-fold). AA-SLNs significantly improved the solubility in PBS at pH 6.8 (88-fold), compared to dH2O (6-fold) and PBS at pH 1.2 (26-fold). In vitro drug release studies showed that OA release from the SLNs was significantly increased within 300 min (p < 0.05) compared to the free drug. Similarly, AA release from the SLNs was significantly increased within 300 min (p < 0.05) compared to free AA. Conclusions: These results demonstrate that SLNs enhance OA and AA solubility and drug release, suggesting a promising strategy for improving oral bioavailability and therapeutic efficacy. Full article
Show Figures

Figure 1

16 pages, 4566 KiB  
Article
Fucoxanthin-Loaded Solid Lipid Nanoparticles Exert Potent Therapeutic Efficacy in Combating High-Fat Diet Induced Obesity in Mice
by Lijun Ding, Xiao Luo and Weijia Wen
Int. J. Mol. Sci. 2025, 26(11), 5249; https://doi.org/10.3390/ijms26115249 - 29 May 2025
Viewed by 596
Abstract
Obesity and associated metabolic disorders pose significant health challenges. Fucoxanthin, a lipophilic compound, has shown promising anti-obesity potential, but its poor solubility and bioavailability limit therapeutic efficacy. The successful formulation of solid lipid nanoparticles (SLNs) amplified fucoxanthin’s efficacy in mitigating obesity and the [...] Read more.
Obesity and associated metabolic disorders pose significant health challenges. Fucoxanthin, a lipophilic compound, has shown promising anti-obesity potential, but its poor solubility and bioavailability limit therapeutic efficacy. The successful formulation of solid lipid nanoparticles (SLNs) amplified fucoxanthin’s efficacy in mitigating obesity and the associated metabolic dysregulation. High-fat diet (HFD)-induced obese mice were treated with free fucoxanthin, lyophilized SLNs (L-SLN), and dispersed SLNs (D-SLN) loaded with fucoxanthin. The intervention with D-SLN demonstrated the most significant reduction in body weight gain (29.94%) and fat mass gain (61.80%) compared to the HFD group (p < 0.05), alongside notable improvements in metabolic indicators including fasting blood glucose, liver enzymes, lipid profile, and inflammatory markers such as leptin and monocyte chemoattractant protein 1 (MCP-1) levels. Histopathological evaluation corroborated these findings, showing highly reduced hepatic lipid droplet accumulation and improved adipocyte and testicular morphology. This advancement paved the way for translating fucoxanthin into a clinically effective anti-obesity agent. Full article
Show Figures

Figure 1

25 pages, 2733 KiB  
Review
Liposomal and Lipid-Based Drug Delivery Systems: Bridging Gut Microbiota and Pediatric Disorder Treatments
by Raluca Ioana Teleanu, Elena-Theodora Moldoveanu, Adelina-Gabriela Niculescu, Elena Predescu, Eugenia Roza, Iulia Florentina Tincu, Alexandru Mihai Grumezescu and Daniel Mihai Teleanu
Pharmaceutics 2025, 17(6), 707; https://doi.org/10.3390/pharmaceutics17060707 - 28 May 2025
Cited by 1 | Viewed by 891
Abstract
The intestine is an important segment of the gastrointestinal tract, which is involved in complex processes that maintain the body’s normal homeostasis. It hosts a vast, diverse, and dynamic microbial community called the gut microbiota, which develops from birth. It has been observed [...] Read more.
The intestine is an important segment of the gastrointestinal tract, which is involved in complex processes that maintain the body’s normal homeostasis. It hosts a vast, diverse, and dynamic microbial community called the gut microbiota, which develops from birth. It has been observed that the gut microbiota is involved in essential physiological processes, including the development of the central nervous system via the gut microbiota–brain axis. An alteration of the gut microbiota can lead to serious health problems, including defective neurodevelopment. Thus, this paper aims to highlight the most recent advances in studies that focus on the link between the gut microbiota and the evolution of neurodevelopmental diseases in children. Currently, studies show that the use of drugs that stimulate and restore the gut microbiota (e.g., probiotics and prebiotics) have the potential to alleviate some of the symptoms associated with conditions such as Autism Spectrum Disorder, Attention Deficit Hyperactivity Disorder, Tic Disorder, Tourette Syndrome, epilepsy, and Down Syndrome. In addition, due to the challenges associated with drug administration in children, as well as the widespread shortage of medications intended for pediatric use, researchers are working on the development of new delivery systems. Liposome-based systems or solid lipid nanoparticles have been safely used for drug delivery in various pediatric conditions, which may also indicate their potential for use in the administration of microbiota-modulating therapies. Full article
(This article belongs to the Special Issue Advanced Liposomes for Drug Delivery, 2nd Edition)
Show Figures

Figure 1

26 pages, 3983 KiB  
Article
Process Analytical Strategies for Size Monitoring: Offline, At-Line, Online, and Inline Methods in a Top-Down Nano-Manufacturing Line
by Christina Glader, Ramona Jeitler, Yan Wang, Remy van Tuijn, Albert Grau-Carbonell, Carolin Tetyczka, Steve Mesite, Philippe Caisse, Johannes Khinast and Eva Roblegg
Pharmaceutics 2025, 17(6), 684; https://doi.org/10.3390/pharmaceutics17060684 - 22 May 2025
Viewed by 791
Abstract
Background/Objectives: Continuous manufacturing is gaining importance in the nanopharmaceutical field, offering improved process efficiency and product consistency. To fully leverage its potential, the integration of Process Analytical Technology (PAT) tools is essential for real-time quality control and robust process monitoring. Among the [...] Read more.
Background/Objectives: Continuous manufacturing is gaining importance in the nanopharmaceutical field, offering improved process efficiency and product consistency. To fully leverage its potential, the integration of Process Analytical Technology (PAT) tools is essential for real-time quality control and robust process monitoring. Among the critical quality attributes (CQAs) of nanosystems, particle size plays a key role in ensuring product consistency and performance. However, real-time size monitoring remains challenging due to complex process dynamics and nanosystem heterogeneity. Methods: This study evaluates the applicability of conventional Dynamic Light Scattering (DLS) and spatially resolved DLS (SR-DLS) using the NanoFlowSizer (NFS) as PAT tools in a temperature-regulated top-down nano-production line. Various lipid-based nanosystems, including solid lipid nanoparticles (SLN), nanostructured lipid carriers (NLC), and nanoemulsions (NEs), were investigated. To ensure reliable implementation, key factors such as sample dilution, viscosity, focus position, measurement angle and temperature effects were systematically assessed for offline and at-line DLS using the Litesizer 500, as well as for offline, inline, and online SR-DLS using the NFS. Results: Offline screening confirmed that selecting the appropriate dilution medium and rate ensures measurement reliability. At-line methods provided an efficient alternative by enabling rapid final product control with minimal manual intervention. Inline and online monitoring further enhanced process efficiency by enabling real-time tracking of size, reducing waste, and allowing immediate process adjustments. Conclusions: This study demonstrates that integrating offline, at-line, in-line, and online DLS techniques allows for comprehensive product monitoring throughout the entire production line. This approach ensures a streamlined process, enables real-time adjustments, and facilitates reliable quality control after production and during storage. Full article
(This article belongs to the Section Pharmaceutical Technology, Manufacturing and Devices)
Show Figures

Graphical abstract

Back to TopTop