Formulation And Optimization Of 5-Fluorouracil Nanosponges Incorporated Topical Gel For Controlled Drug Delivery
Keywords:
5-Fluorouracil; Nanosponges; Carbopol 934; Topical gel; Box–Behnken design; Controlled drug delivery; Drug release; Entrapment efficiency; Skin irritation; StabilityAbstract
The present study was aimed at the development and evaluation of 5-Fluorouracil (5-FU) loaded nanosponges gel for controlled topical drug delivery. Preformulation studies of 5-FU included physical appearance, solubility, melting point, wavelength maximum, calibration curve, and drug–excipient compatibility studies by FTIR and DSC. 5-FU loaded nanosponges were prepared and optimized using a Box–Behnken design, with ethyl cellulose, PVA, and stirring time as formulation variables. Entrapment efficiency and particle size were selected as response variables. The optimized nanosponge formulation F13 showed 90.25% entrapment efficiency, 121.80 nm particle size, and −38.45 mV zeta potential. The optimized nanosponges were incorporated into Carbopol 934 gel to prepare six formulations (NG1–NG6) containing different polymer concentrations. The prepared gels were evaluated for appearance, after-feel, consistency, homogeneity, pH, drug content, spreadability, viscosity, and in-vitro drug release. The formulations exhibited satisfactory physicochemical characteristics, with pH ranging from 6.21 ± 0.20 to 6.82 ± 0.18 and drug content from 95.65 ± 0.35% to 98.25 ± 0.28%. Increasing Carbopol 934 concentration resulted in increased viscosity and reduced spreadability, with a corresponding retardation of drug release. Drug-release kinetics were evaluated using zero-order, first-order, Higuchi, and Korsmeyer–Peppas models. Skin irritation studies showed no visible skin reaction. Stability studies of the optimized NG4 formulation demonstrated only minor changes in physical characteristics, pH, and drug content during storage. The developed 5-FU nanosponges gel demonstrated satisfactory physicochemical properties, controlled drug-release behavior, skin compatibility, and stability, indicating its potential as a topical controlled drug delivery system....
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