Background: The rise of pathogenic fungi capable of infecting people is a major public health problem. Flucytosine is an effective antifungal agent, but its clinical use is constrained by rapid clearance and dose-related adverse effects. Nanoemulsion-based systems offer a promising strategy for drug delivery and therapeutic performance. The objective of this work was to develop and optimize a flucytosine-loaded nanoemulsion using a Quality by Design (QbD) approach based on the Box-Behnken design, and to evaluate its physicochemical characteristics. Methodology: A Box-Behnken design (BBD) was used to optimize formulation factors, including lipid concentration, Smix (surfactant-to-cosurfactant) ratio, and homogenization time, using high-speed homogenization. The impacts on particle size, polydispersity index, and entrapment efficiency (EE) were investigated. UV-visible spectroscopy, Fourier-transform infrared spectroscopy (FTIR), and X-ray diffraction (XRD) were used to assess the compatibility and stability of the improved formulation (F11) with the chosen excipients. Results and Discussion: The optimized formulation (F11) had a particle size of 318.18 nm and a PDI of 0.136, a zeta potential of -22.2 mV, and high entrapment efficiency (96.36%), indicating good stability and uniformity. Preformulation and compatibility studies confirmed the absence of drug-excipient interactions. Statistical analysis demonstrated that formulation variables significantly influenced critical quality attributes. Conclusion: The study demonstrates that QbD-driven optimization can successfully develop a stable and efficient flucytosine nanoemulsion with enhanced drug-loading capacity and potential to improve antifungal therapy. However, further studies, including in vitro drug release, in vivo evaluation, long-term stability, and clinical validation, are required to confirm its performance in drug delivery applications.
Rajat Srivastava, A. Rawat· Journal of Applied Pharmaceu...· 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
