TL;DR
It is suggested that RST-loaded chitosan nanoparticles represent a promising oral nanocarrier system with sustained release characteristics and the potential to improve the oral performance of poorly water-soluble drugs such as rosuvastatin calcium.
BACKGROUND Pitavastatin (PVN), a BCS class-II drug, exhibits poor aqueous solubility leading to limited oral bioavailability and therapeutic efficacy. OBJECTIVES This study aimed to enhance the solubility and anti-hyperlipidemic efficacy of Pitavastatin (PVN) by encapsulating it in chitosan-based polymeric nanoparticles. METHODS Pitavastatin-loaded chitosan nanoparticles (NPs) were prepared using the ionic gelation method. Formulations were characterized by particle size, zeta potential, drug loading, In-vitro drug release and surface morphology. Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), thermal analysis (TGA and DSC), ex-vivo intestinal permeability and in-vivo pharmacodynamic analysis were also performed. RESULTS The size of PVN-loaded NP ranged from 219.9±1.11 to 292.7±2.29 nm with PDI 0.2-0.4, surface charge of +28.4 ± 0.43 to 32.5 ± 1.02 mV and entrapment efficiency 65±1.12-93±1.23%. Solubility in different media (PBS (pH 6.8), 0.1N HCl (pH 1.2) and distilled water showed a 56-102-fold increase compared to PVN. SEM analysis revealed a smooth surface and spherical geometry of the NP. FTIR analysis confirmed that there was no physicochemical interaction between PVN and chitosan in NP formulations (NP1-NP5). XRD and thermal analysis indicated the amorphous nature of PVN-loaded NP. In-vitro drug release from NP formulations (NPI-NP5) ranged from 80.97±4.80 to 81±3.90% indicating sustained release, while ex-vivo intestinal permeability was 1.5-fold higher than PVN. The optimized formulation (NP1) followed Higuchi release model, indicating Fickian diffusion. Pharmacodynamic analysis of lipid profiles in hyperlipidemic albino rats suggested that NP1 reduced low-density lipoprotein (LDL) by 33±1.24 %, total cholesterol by 29±2.13% and triglycerides by 23±1.21%, showing better results than PVN. CONCLUSION Chitosan-based Pitavastatin nanoparticles successfully enhanced drug solubility and provided sustained release, leading to improved ex-vivo permeability and greater in-vivo anti-hyperlipidemic activity in albino rats. This approach represents a promising strategy for enhancing therapeutic potential of Pitavastatin.
The present study aimed to develop and evaluate Anastrozole-loaded mucoadhesive microspheres for sustained oral drug delivery using Sodium CMC, Chitosan, and HPMC K4M polymers. Microspheres were prepared by the solvent evaporation method and characterized for their micromeritic properties, percentage yield, drug entrapment efficiency, swelling behavior, mucoadhesion, surface morphology, and in vitro drug release. The prepared formulations exhibited satisfactory flow properties with particle sizes ranging from 420.15 to 468.41 µm. Percentage yield and drug entrapment efficiency were found to be in the ranges of 88.31–99.52% and 87.14–99.82%, respectively. The microspheres demonstrated excellent swelling and mucoadhesive characteristics, indicating their suitability for prolonged gastrointestinal residence. In vitro dissolution studies revealed sustained drug release for up to 12 h, with cumulative drug release ranging from 85.87% to 99.92%. Among all formulations, A6 containing Chitosan at a drug-to-polymer ratio of 1:2 showed the most desirable performance, achieving 99.92% drug release with superior mucoadhesion and controlled-release characteristics. FTIR studies confirmed the absence of significant drug–polymer interactions, while SEM analysis revealed discrete and spherical microspheres with smooth surface morphology. Drug release kinetic analysis demonstrated that the optimized formulation followed Zero-order kinetics with a non-Fickian diffusion mechanism. The findings suggest that Chitosan-based Anastrozole microspheres are a promising sustained-release oral delivery system capable of improving therapeutic efficacy and patient compliance in breast cancer management.
Findings establish chitosan-coated, cholesterol-Tween niosomes as versatile, biocompatible carriers that provide sustained release and preserve bioactivity, with promising potential for ocular drug delivery and broader biomedical applications.
INTRODUCTION/OBJECTIVE Letrozole (LTZ)-loaded polymeric nanoparticles (PNPs) were formulated with Eudragit® RS100 to investigate their potential as a preliminary drug delivery system for hepatocellular carcinoma (HCC). METHODS Nanoparticles were prepared using the spray-drying technique with a Büchi B-90 Nano Spray Dryer and characterized in terms of morphology, particle size, polydispersity index (PDI), zeta potential, drug loading efficiency, thermal and structural characteristics, in vitro release behavior, and preliminary cytotoxicity. RESULTS SEM analysis demonstrated the formation of predominantly spherical particles with relatively smooth surfaces. The prepared nanoparticles exhibited initial particle sizes ranging between 253 nm and 425 nm, with PDI values of 0.3-0.4 and positive zeta potential values between 36 and 48 mV. Encapsulation efficiency (EE%) and drug loading (DL%) values were determined as 47.9%-56.9% and 9.1%-18.6%, respectively. Thermal and structural analyses indicated the molecular dispersion of LTZ within the polymeric matrix. In vitro release studies conducted at pH 7.4 demonstrated an initial burst release, followed by a sustained drug release profile over 24 h, with cumulative drug release reaching almost 80%. The preliminary cytotoxicity of the formulations was evaluated using the methylthiazolyl-diphenyl-tetrazolium bromide (MTT) assay on human hepatocellular carcinoma (HepG2) and healthy human dermal fibroblast (BJ) cell lines. Free LTZ demonstrated an IC50 value of 142.76 µg/mL against HepG2 cells, whereas the optimized nanoparticle formulation exhibited an IC50 value higher than 121.85 µg/mL. DISCUSSION The obtained results confirmed the successful development of LTZ-loaded polymeric nanoparticles with suitable physicochemical properties, efficient drug encapsulation, and sustained release behavior. The positive surface charge and nanoscale size may support formulation stability. Furthermore, the nanoparticles preserved the cytotoxic activity of LTZ, indicating their potential as an effective drug delivery system. CONCLUSION Overall, the findings suggest that the developed nanoparticles constitute a promising drug delivery system for further investigation in HCC-related therapy. However, additional mechanistic studies and in vivo evaluations are required to comprehensively assess their true therapeutic potential.
Objective: The present study aimed to formulate and evaluate a diosmin-loaded niosomal gel for enhanced topical anti-inflammatory activity. Methods: Diosmin, a natural flavonoid with poor solubility and limited bioavailability, was encapsulated into non-ionic surfactant-based niosomes using the thin-film hydration method. Various formulations (DF1–DF10) were developed by varying the concentrations of Span 60 and cholesterol to optimise vesicle characteristics (Entrapment efficiency, particle size, in vitro drug release, zeta potential). Results: The optimised formulation (DF10) exhibited an entrapment efficiency of 86.85±0.06%, a particle size of 292.5±0.7 nm, a polydispersity index (PDI) of 0.403±0.23, and a zeta potential of –24.7 mV±0.13, indicating stable, uniform vesicles. SEM analysis confirmed spherical morphology with smooth surfaces. In vitro release studies showed sustained drug release of 96.34±0.15% over 24 h. The optimized niosomal dispersion was incorporated into a Carbopol 934 gel base, neutralised with triethanolamine to form a clear, stable niosomal gel. The prepared gel exhibited desirable physicochemical properties, including a pH of 6.3±1.04, viscosity of 36,000±1.04 cP, spread ability of 20.4 g·cm/sec, and drug content of 98.5±1.02%. In vitro diffusion studies demonstrated controlled, prolonged release (95.34±0.15 % at 24 h), following zero-order kinetics with a non-Fickian mechanism, suggesting a combination of diffusion and polymer relaxation. Conclusion: The developed diosmin-loaded niosomal gel showed potential for sustained drug delivery, improved skin permeation, and enhanced therapeutic efficacy for topical anti-inflammatory treatment.
Background: Topical drug delivery systems provide site-specific therapy with reduced systemic exposure. Nanosponges have emerged as promising carriers owing to their porous structure, enabling improved drug stability, bioavailability, and sustained release. Apremilast, a phosphodiesterase-4 (PDE4) inhibitor with anti-inflammatory activity, has potential for topical wound management when formulated as a controlled-release delivery system. Methods: Apremilast-loaded nanosponges were prepared by the emulsion solvent diffusion method using Ethyl Cellulose (EC) and Polyvinyl Alcohol (PVA). A 3² factorial design was used to optimize the EC: PVA ratio and sonication time. Formulations were evaluated for particle size, entrapment efficiency, zeta potential, in vitro drug release, and surface morphology. Characterization included UV spectroscopy, FTIR, XRD, DSC, and SEM. Drug release kinetics were analyzed using mathematical models. Results: Preformulation studies confirmed drug purity and compatibility with excipients. The optimized formulation (NS8) exhibited a particle size of 213.85 nm, an entrapment efficiency of 82.75%, a zeta potential of −33.3 mV, and a sustained drug release of 95.85% over 24 h. SEM revealed spherical porous nanosponges, while FTIR, XRD, and DSC confirmed drug integrity and formulation stability. Response surface analysis demonstrated significant effects of formulation variables on performance. Drug release followed the Higuchi model (R² = 0.987), and the Korsmeyer–Peppas exponent (n = 0.58) indicated anomalous non-Fickian diffusion. Conclusion: Apremilast-loaded nanosponges demonstrated sustained drug release, excellent stability, and favorable physicochemical characteristics, indicating their potential as an effective topical delivery system for wound management. Further ex vivo, in vivo, and clinical studies are required to confirm therapeutic efficacy and safety.