Therapeutic delivery最新文献

Poly (vinyl alcohol) (PVA) nanofibers are emerging as aqueous-processable, biocompatible platforms for drug delivery, wound care, and tissue engineering. This review synthesizes advances in electrohydrodynamic fabrication - including classic single-fluid spinning and its melt, coaxial, emulsion, air-blown, and multilayer variants - and maps how solution properties and processing parameters translate into fiber morphology, stability, and performance. We highlight formulation strategies (chemical/physical crosslinking, blending, and compartmentalized core - sheath or multilayer architectures) that leverage PVA's hydrophilicity to yield tunable water-responsiveness and release kinetics for small molecules, biologics, and combination products. On the application side, we summarize evidence across oral, transdermal, pulmonary, and transmucosal delivery, as well as scaffold-guided regeneration and device coatings. Persistent bottlenecks are also reviewed: spinneret clogging, morphology control, rapid aqueous dissolution, and low per-nozzle throughput; we outline industrialization pathways - needleless/free-surface, multi-jet, centrifugal (forcespinning), and roll-to-roll lines - that can raise productivity while improving uniformity and safety. Finally, we discuss translation: the current lack of inhalation-route excipient approval for PVA, route-specific toxicology requirements, and drug - device co-development considerations, alongside market signals and the need for GMP-ready, scalable processes. We conclude that PVA nanofibers offer a versatile, regulation-conscious platform whose progress will hinge on scalable manufacturing, durability under wet use, and rigorous, application-relevant characterization.

Aim: This study evaluated two novel combination therapies using 5-Fluorouracil (5-FU), Thymoquinone (TQ), and cockle shell - derived calcium carbonate nanoparticles (CaCO₃ NPs) against HT-29 colorectal cancer (CRC) cells under hyperglycemic conditions.

Methods: 5-FU and TQ were successfully encapsulated into CaCO₃ NPs through encapsulation at various drug-to-nanoparticle ratios. Physicochemical characterization was performed to confirm the morphology, and particle stability. Drug release studies assessed pH-responsive behavior, while biocompatibility was evaluated on NIH/3T3 cells. Cytotoxicity and cell cycle analyses were conducted on HT-29 cells under glycemic and hyperglycemic conditions.

Results: High encapsulation efficiency was achieved at a 1:5 drug-to-nanoparticle ratio while maintaining the aragonite structure and stable physicochemical properties. The nanoformulations exhibited pH-sensitive drug release with enhanced release at acidic pH (4.8), simulating the tumor microenvironment. Improved biocompatibility and reduced toxicity were observed in normal NIH/3T3 cells compared to free drugs. Both 5-FU:TQ-CaCO₃ NPs and 5-FU-CaCO₃ NPs:TQ combinations significantly inhibited HT-29 proliferation and induced G1 cell cycle arrest, especially under hyperglycemic conditions. Combination index analysis confirmed synergistic effects of both treatments.

Conclusion: The findings suggest the potential therapeutic efficacy of 5-FU:TQ-CaCO₃ NPs and 5-FU-CaCO₃ NPs:TQ in treating CRC associated with hyperglycemia and demonstrate the capability of biogenic CaCO₃ NPs to effectively deliver chemotherapeutic agents of different polarity with minimal toxicity.

Comprehensive nanoparticle (NP) characterization and its interactions with cells are critical for the successful development of effective drug delivery systems (DDS). In this context, atomic force microscopy (AFM), a high-resolution technique, provides relevant information about NP properties, such as topography, size, stiffness, and viscoelasticity at the nanoscale level. The knowledge and correlation of these parameters enable rational design of NPs with tailored and controlled properties to target specific cells and/or tissues, making AFM a powerful tool for nanotechnology research. This review explores and discusses the features of AFM in providing high-resolution images of NP surfaces, as well as size and mechanical properties measurements. Through critical analysis, the challenges and limitations inherent in AFM-based NP characterization (e.g. tip convolution, slow acquisition speed, and sample preparation artifacts) are addressed, and the correlation between mechanical properties of NPs with their interactions in biological systems is discussed. This review adopts a broad approach, aiming to guide researchers in experimental design and to provide an updated perspective on the applicability and advancements of AFM in the drug delivery field.

Aims: The aim of this study was to prepare different silica-based hydrogel composites and to study how the amount and type of silica particles - both with and without embedded APIs - can be varied in presence of alginate in the hydrogel composites, and its influence on the rheological properties and dissolution rates.

Materials and methods: Silica microparticles with and without encapsulated levothyroxine were manufactured from alkoxide hydrolysis and spray drying to be subsequently mixed with silica hydrogel in the presence and absence of small amounts of sodium alginate. The resulting material was treated under in-sink conditions to evaluate the dissolution rates. In addition, the obtained material was tested for rheology and injection force measurements.

Results: The findings demonstrate that alginate facilitates the reduction of silica microparticle concentration while maintaining injectability and modulating dissolution rates, thereby enhancing formulation tunability. Furthermore, alginate improved the rheological characteristics and injection performance of composites containing levothyroxine-loaded silica microparticles, which otherwise posed injection difficulties.

Conclusions: The study had shown that alginate contributes to the formation of more homogeneous hydrogel silica composites under shear stress, supporting its potential as a functional excipient in advanced drug delivery systems.

Aim: This study aimed to evaluate a range of cosolvents and their mixtures as liquid vehicles to enhance the solubility and trypanocidal efficacy of nifurtimox.

Materials & methods: Several pharmaceutical-grade solvents were screened for their ability to solubilize nifurtimox. The cytotoxicity of selected cosolvent systems was assessed and analyzed using the hemolysis assay. The stability of nifurtimox in these systems was studied under various temperature conditions. The trypanocidal activity of nifurtimox formulated in cosolvent systems was tested against Trypanosoma cruzi trypomastigotes by determining the drug concentration required to lyse 50% of the parasite population.

Results: Nifurtimox solubility increased from 0.2 mg/mL in water to 23.5 mg/mL in selected cosolvent systems. Hemolytic assays indicated acceptable cytotoxicity profiles for the most promising formulations, supporting their suitability for further development. Trypanocidal studies demonstrated that these systems effectively inhibited or killed Trypanosoma cruzi trypomastigotes. Stability studies confirmed that nifurtimox solutions remained chemically stable, with no precipitation and consistent drug content at all tested storage temperatures.

Conclusion: Cosolvent-based delivery systems enhance the solubility of nifurtimox while maintaining adequate trypanocidal activity against Trypanosoma cruzi and demonstrating acceptable stability and safety profiles. Thus, these formulations represent a promising strategy to improve the therapeutic effectiveness of nifurtimox.

Aims: To develop and evaluate α-Cyperone (α-Cy)-loaded solid lipid nanoparticles (SLNs) incorporated into a thermosensitive in situ gel for enhanced intranasal delivery and improved neuroprotective efficacy.

Materials and methods: α-Cy-SLN was prepared using high-pressure homogenization followed by freeze-drying. The formulation was optimized using a Box-Behnken Design, assessing the effects of lipid-to-surfactant ratio on particle size, polydispersity index (PDI), zeta potential, and entrapment efficiency (EE). The optimized SLNs were characterized for physicochemical properties, in vitro drug release, and brain cell penetration.

Results: The optimized α-Cy-SLNs (Run 5) exhibited a mean particle size of 279.5 ± 0.06 nm, PDI of 0.203 ± 0.24, zeta potential of -23.1 ± 2.38 mV, EE of 70.0 ± 2.21%, and product yield of 72.58 ± 1.24%. In vitro studies demonstrated a sustained release of α-Cy from the SLNs, indicating the formulation's potential for prolonged drug delivery. Incorporation into the thermosensitive in situ gel further supported controlled release and enhanced bioavailability.

Conclusions: The developed α-Cy-SLN in situ gel formulation offers a promising strategy for intranasal delivery, improving α-Cy bioavailability and therapeutic potential for neuroprotection in Alzheimer's disease.

Nanoparticle encapsulation has emerged as a relevant technology with the potential to revolutionize multiple fields, including medicine, food technology, cosmetics, and environmental monitoring. This review discusses the fundamental aspects of nanoparticle encapsulation, highlighting its benefits, such as enhanced solubility, stability, and bioavailability of phytochemicals. The data for this report were obtained via an extensive review of the peer-reviewed scientific literature. We reviewed various types of nanoparticles used in encapsulation, the efficacy of nanoparticle-encapsulated phytochemicals, and the challenges faced, including formulation complexity and regulatory hurdles. The review also considers current and future applications, providing examples of how advanced technologies such as artificial intelligence and novel manufacturing methods contribute to innovation in this field. As nanoparticle technology progresses, addressing safety and regulatory issues will be critical for its successful integration and commercialization. This review underscores the promising future of nanoparticle technology.

Background: Type 2 diabetes mellitus (T2DM) is the most devastating disease and it necessitates therapeutic intervention for its effective management. Human Glucagon-like peptide-1 (HuGLP-1) is the potential candidate in the treatment of T2DM; however, it limits its utilization owing to its solubility and stability issues.

Aims: The current investigation aims to develop HuGLP-1-loaded bilosomes as a novel strategy for managing T2DM.

Materials and methods: The HuGLP-1-loaded bilosomes were developed and characterized for its size, polydispersity index, surface charge, entrapment efficiency, morphology, drug release, and stability studies. The hypoglycemic potential and histopathology were studied using streptozotocin-induced diabetic rats.

Results: Bilosomes were successfully developed with size of 197.96 ± 0.61 nm, polydispersity index 0.191 ± 0.01 and surface charge of -27.63 ± 1.02 mV. The in vitro release of HuGLP-1-loaded bilosomes showed sustained release profile of HuGLP-1 extending over 24-h period, in compared to plain HuGLP-1 solution, and follows Weibull release kinetics model. The HuGLP-1-loaded bilosomes revealed significant hypoglycemic effects in comparison to both oral and subcutaneous HuGLP-1 solutions. Histopathological evaluations revealed that HuGLP-1-loaded bilosomes showed promising improvement in histology of liver, kidney, and intestines.

Conclusion: The HuGLP-1-loaded bilosomes were found to be potential therapeutic approach for the effective management of T2DM.