2025· Bio-Research· Vol 23, pp. 238-245· 0 citations
TL;DR
The combined findings indicate that chitosan coating improved the physicochemical characteristics of simvastatin while providing sustained release potential, and chitosan-coated simvastatin nanoparticles represent a promising oral nanocarrier system for enhancing simvastatin delivery and therapeutic performance.
Abstract
Simvastatin is an effective antihyperlipidemic agent whose clinical utility is limited by poor aqueous solubility, low gastrointestinal absorption, and extensive first-pass metabolism, resulting in reduced oral bioavailability. This study aimed to formulate and characterize chitosan-coated simvastatin nanoparticles as a strategy to improve its physicochemical performance and controlled release properties. Nanoparticles were prepared using the ionic gelation method involving electrostatic interaction between chitosan and sodium tripolyphosphate. The developed formulation was evaluated by in vitro drug release studies, scanning electron microscopy (SEM), and Fourier transform infrared spectroscopy (FTIR). The release profile demonstrated a biphasic pattern with an initial burst release during the early phase, followed by sustained drug release reaching approximately 70–75% over 300 minutes, indicating effective controlled-release behavior. SEM analysis showed clear morphological transformation from loosely aggregated crystalline simvastatin particles to denser and more cohesive nanoparticulate structures after chitosan coating, confirming successful encapsulation. FTIR spectra retained the characteristic peaks of both simvastatin and chitosan with only minor shifts in band positions, suggesting structural integrity of the drug and absence of significant chemical incompatibility between formulation components. The combined findings indicate that chitosan coating improved the physicochemical characteristics of simvastatin while providing sustained release potential. Therefore, chitosan-coated simvastatin nanoparticles represent a promising oral nanocarrier system for enhancing simvastatin delivery and therapeutic performance.
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.
M. Sarwer, R. M. Sarfraz, Asif Mahmood et al.· BioNanoScience· 0 citations
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.
Sony Moni Das, Z. Fatima, P. Awat et al.· Physical Chemistry, Chemical...· 0 citations
Objective: Paclitaxel is a widely used chemotherapeutic agent with extremely poor aqueous solubility (~0.3 µg/ml), which significantly limits its bioavailability and therapeutic efficacy. The present study aimed to develop and characterize paclitaxel-loaded poly(lactic-co-glycolic acid) (PLGA) nanoparticles to enhance solubility, dissolution behavior, and in vitro anticancer activity.
Methods: Nanoparticles were prepared using the solvent evaporation method and optimized by varying the drug-to-polymer ratio and homogenization conditions. The optimized formulation was characterized for particle size, polydispersity index (PDI), and zeta potential. Differential scanning calorimetry (DSC) and x-ray diffraction (XRD) were used to evaluate the physical state of paclitaxel, while Fourier-transform infrared spectroscopy (FTIR) analysis was performed to assess chemical compatibility between the drug and polymer. Solubility and dissolution studies were conducted, and cytotoxicity was evaluated using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay.
Results: The optimized formulation exhibited an average particle size of 195±5 nm, polydispersity index of 0.11, and zeta potential of −32±2 mV, indicating good colloidal stability. DSC and XRD analysis confirmed the transformation of paclitaxel from crystalline to amorphous form within the polymer matrix. FTIR analysis demonstrated chemical compatibility between the drug and polymer. The nanoparticle formulation significantly enhanced aqueous solubility, achieving approximately a 24-fold increase (from 0.3 µg/ml to 7.2 µg/ml). In vitro dissolution studies revealed sustained drug release with more than 85% release within 24 h, whereas the native drug showed less than 20% release. Cytotoxicity evaluation using the MTT assay demonstrated improved anticancer activity, with reduced IC₅₀ values compared to the native drug.
Conclusion: These findings demonstrate that PLGA-based nanoparticles represent a promising approach for improving the solubility and therapeutic performance of poorly water-soluble anticancer agents.
R. Malkawi· International Journal of App...· 0 citations
INTRODUCTION/OBJECTIVE
Timolol Maleate (TM) is primarily used to treat glaucoma by reducing intraocular pressure. However, its efficacy is limited by poor ocular bioavailability (<5%) and systemic side effects. This study aimed to develop and evaluate Low-Molecular-Weight Chitosan (LMWC)-based complexes in an eye formulation to sustain TM release and enhance its corneal permeability.
METHODS
TM-LMWC Polyelectrolyte Complexes (PECs) were prepared by ionic interactions between TM and LMWC and characterized for particle size, polydispersity, surface charge, and physicochemical properties. TM Liquid Medicated Nanoparticle Formulations (LMFs) were prepared by the solvent diffusion method, and their dissolution behaviors, release kinetics in simulated tear fluid, and ex vivo permeation through sheep corneas were evaluated.
RESULTS
The prepared TM nanoparticles showed a uniform particle size (185-258 nm) and a positive zeta potential exceeding +26 mV, with encapsulation efficiency ranging from 28 to 35%. The formation of a polycationic complex was confirmed by the thermal and structural analyses. The LMFs showed a reduced particle size (65-130 nm). Moreover, the TEM image of LMF 4 revealed a spherical nanoparticle with a smooth surface. Sustained drug release was observed over 24 hours and best fitted to the Korsmeyer-Peppas model, indicating a Fickian diffusion (n < 0.45). Ex vivo studies showed LMF1 increased flux (2.54 ± 0.04 μg cm-2 h-1) and permeation coefficient (0.00987 cm·h⁻¹), representing a 2.62-fold increase in TM permeation.
DISCUSSION
Chitosan molecular weight influenced PEC particle size due to differences in polymer chain length and viscosity. A sustained release of TM from LMFs was observed as TM was entrapped within the chitosan matrix and had to diffuse through the polymer or be released by matrix erosion. The enhanced corneal permeability was attributed to the mucoadhesive properties of the nanoparticles and their interaction with the corneal epithelium.
CONCLUSION
The TM-based nanoparticle formulation enhanced corneal permeation and sustained TM release, offering a promising approach to improve ocular bioavailability and therapeutic efficacy.
Areen Alshweiat, S. O. Emran, Bashar Altaani et al.· Current Drug Delivery· 0 citations
Oxiconazole nitrate-loaded nanospheres were successfully developed using the emulsification–solvent evaporation method to enhance the solubility and dissolution of oxiconazole nitrate, a Biopharmaceutics Classification System (BCS) Class II antifungal drug characterized by low aqueous solubility and good membrane permeability. Oxiconazole exerts its antifungal activity by inhibiting lanosterol 14-α-demethylase (CYP51), thereby disrupting ergosterol biosynthesis, compromising fungal cell membrane integrity, and ultimately causing cell lysis. Eudragit RS 100 was employed as the polymeric carrier, with methanol serving as the solvent. The prepared nanospheres were evaluated for particle size, percentage yield, entrapment efficiency, solubility enhancement, Fourier-transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), differential scanning calorimetry (DSC), zeta potential, and in vitro drug-release characteristics. Among the formulations, batch F5 demonstrated optimum performance, exhibiting an entrapment efficiency and percentage yield of 83.40%, an average particle size of 11.8 nm, and enhanced aqueous solubility in phosphate buffer (pH 7.4). FTIR and DSC analyses confirmed the absence of significant drug–polymer interactions and demonstrated the thermal stability of the formulation. The optimized formulation exhibited a zeta potential of −80.9 mV, indicating excellent colloidal stability. Furthermore, the nanosphere gel (G2) achieved 98.13% drug release within 6 hours, confirming that nanosphere formulation significantly improved the solubility and dissolution behaviour of oxiconazole nitrate.
Suyash Shashikant Ingle, Asmita Vilas Chavan, Vasundhara Somnath Patil et al.· International Journal of Sci...· 0 citations
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.
Purnima Rai, A. Rawat· Journal of Applied Pharmaceu...· 0 citations