Preparation, Characterization and Evaluation of Loteprednol Etabonate Microemulsion for Ocular Delivery
XU Ruo-xuan, WU Yu-ying, KE Xue*
Department of Pharmaceutics, China Pharmaceutical University, Jiangsu Public Technical Service Center for Nanometer Drug Preparation and Biological Evalution, Nanjing 210009, China
Abstract：OBJECTIVE To prepare loteprednol etabonate (LE) ophthalmic microemulsion and improve the efficacy. METHODS The optimum oil phase, emulsifier and coemulsifier and their contents were selected by solubility, emulsifying ability and pseudo ternary phase diagram. Its physical and chemical properties, microstructure, in vitro release ability and corneal permeability were investigated, and the ocular pharmacodynamics was preliminarily evaluated. RESULTS The best formulation of LE ophthalmic microemulsion was obtained. Its particle size, PDI and other physical and chemical properties were good. The in vitro release results showed that LE microemulsion released faster and more completely than suspension eye drops. The corneal penetration of microemulsion was more than that of suspension eye drops, and the penetration rate was faster.Pharmacodynamic studies showed that the cure time of LE ophthalmic microemulsion was shorter than that of suspension eye drops, indicating that LE microemulsion improved the efficacy. CONCLUSION The prepared LE ophthalmic microemulsion has the characteristics of simple process, fast onset and long-lasting release, which can improve the efficacy of the drug and is suitable for ocular administration.
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2023, Vol. 58 
