The present study aimed to develop and evaluate a flucytosine-loaded invasomal gel for improved topical antifungal drug delivery. Nine invasomal formulations (F1–F9) were prepared by varying terpene and phosphatidylcholine concentrations while maintaining flucytosine concentration at 1% w/v. The prepared invasomes were evaluated for entrapment efficiency and vesicle size. Among the formulati1ons, F9 exhibited the highest entrapment efficiency of 89.48% and the lowest vesicle size of 178.4 nm and was selected as the optimized invasome. The optimized invasomes were incorporated into Carbopol 934 gel at different polymer concentrations to prepare IG-1, IG-2 and IG-3. The formulations were evaluated for viscosity, pH, drug content, extrudability and spreadability. IG-2 demonstrated a suitable combination of physicochemical properties, with viscosity of 3924 ± 18 cps, pH 5.89 ± 0.02, drug content 99.46 ± 0.21%, extrudability 178 ± 2 g and spreadability 11.64 ± 0.27 g·cm/s, and was selected as the optimized invasomal gel. In-vitro drug-release studies showed sustained release from IG-2, with 89.46% cumulative drug release at 12 h compared with 88.65% release of pure flucytosine within 5 h. The release kinetics showed the highest correlation with the first-order and Higuchi models (R² = 0.9892), indicating an important contribution of diffusion to drug release. The optimized gel also exhibited enhanced antifungal activity against Candida albicans, producing zones of inhibition of 15.62 ± 0.24, 21.48 ± 0.29 and 27.36 ± 0.31 mm at 10, 20 and 30 µg/mL, respectively, compared with 12.36 ± 0.28, 16.74 ± 0.32 and 20.58 ± 0.35 mm for pure flucytosine. Stability studies further demonstrated satisfactory physical stability of IG-2 for six months at 4 ± 2°C and 25 ± 2°C. The findings indicate that the flucytosine-loaded invasomal gel may serve as a promising topical delivery system providing sustained drug release and enhanced antifungal activity. Keywords: Flucytosine, Invasomes, Invasomal gel, Carbopol 934, Topical drug delivery, Sustained drug release, Candida albicans, Antifungal activity.
Manu Kumar Singh*, Dr. Sandesh Asati, Dr. Brijesh Sirohi, Dr. Vishnu Raj· Zenodo (CERN European Organi...· 0 citations
The present study aimed to develop and evaluate a flucytosine-loaded invasomal gel for improved topical antifungal drug delivery. Nine invasomal formulations (F1–F9) were prepared by varying terpene and phosphatidylcholine concentrations while maintaining flucytosine concentration at 1% w/v. The prepared invasomes were evaluated for entrapment efficiency and vesicle size. Among the formulati1ons, F9 exhibited the highest entrapment efficiency of 89.48% and the lowest vesicle size of 178.4 nm and was selected as the optimized invasome. The optimized invasomes were incorporated into Carbopol 934 gel at different polymer concentrations to prepare IG-1, IG-2 and IG-3. The formulations were evaluated for viscosity, pH, drug content, extrudability and spreadability. IG-2 demonstrated a suitable combination of physicochemical properties, with viscosity of 3924 ± 18 cps, pH 5.89 ± 0.02, drug content 99.46 ± 0.21%, extrudability 178 ± 2 g and spreadability 11.64 ± 0.27 g·cm/s, and was selected as the optimized invasomal gel. In-vitro drug-release studies showed sustained release from IG-2, with 89.46% cumulative drug release at 12 h compared with 88.65% release of pure flucytosine within 5 h. The release kinetics showed the highest correlation with the first-order and Higuchi models (R² = 0.9892), indicating an important contribution of diffusion to drug release. The optimized gel also exhibited enhanced antifungal activity against Candida albicans, producing zones of inhibition of 15.62 ± 0.24, 21.48 ± 0.29 and 27.36 ± 0.31 mm at 10, 20 and 30 µg/mL, respectively, compared with 12.36 ± 0.28, 16.74 ± 0.32 and 20.58 ± 0.35 mm for pure flucytosine. Stability studies further demonstrated satisfactory physical stability of IG-2 for six months at 4 ± 2°C and 25 ± 2°C. The findings indicate that the flucytosine-loaded invasomal gel may serve as a promising topical delivery system providing sustained drug release and enhanced antifungal activity. Keywords: Flucytosine, Invasomes, Invasomal gel, Carbopol 934, Topical drug delivery, Sustained drug release, Candida albicans, Antifungal activity.
Manu Kumar Singh*, Dr. Sandesh Asati, Dr. Brijesh Sirohi, Dr. Vishnu Raj· Zenodo (CERN European Organi...· 0 citations
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