Preparation and Quality Evaluation of Butenafine Hydrochloride Thermosensitive Microemulsion-Based Hydrogel / 中国药学杂志

ABSTRACT

OBJECTIVE: To prepare butenafine hydrochloride thermosensitive microemulsion-based hydrogel and evaluate the quality. METHODS: A series of temperature sensitive microemulsion gels with different gelation temperatures were prepared, using ethyl oleate as oil phase, Tween 80 as surfactant, ethanol as co-surfactant, and poloxamer as temperature-sensitive material. The morphology, particle size, Zeta potential, percutaneous absorption speed and skin retention were evaluated. RESULTS: The best formulation was composed of ethyl oleate-Tween 80-ethanol-poloxamer 407-poloxamer 188-distilled water at ratios of 4∶15∶10∶16.33∶5.68∶71. The oil/water microemulsion exhibited a spherical shape without adhesion or aggregation observed by TEM. The average diameter was 91.03 nm and the PDI was 0.246. The transdermal speed of microemulsion gel was faster than the marketed cream, and the drug retention in the skin was 5 times of the marketed cream. CONCLUSION: The hydrogel exhibits good temperature sensitivity and skin retention effect, and can penetrate skin cutin and act as a depot thus increase the local drug concentration and enhance the antibacterial effect.