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目的:以维生素A棕榈酸酯(VAP)为模型,制备N-三甲基壳聚糖(TMC)包衣的眼用阳离子脂质体-原位凝胶,研究其角膜滞留特性,并评价其角膜刺激性。方法:采用薄膜分散法结合冰水浴搅拌制备TMC包衣的VAP脂质体-原位凝胶(VAPL-ISG),采用悬挂泡和束缚泡技术进行离体眼球表面解吸附动力学研究,Draize评分法评价对兔角膜刺激性。结果:透射电镜显示VAPL-ISG粒径分布均匀,经包衣后荷正电性。与诺沛凝胶和未包衣的VAPL-ISG相比,TMC包衣的VAPL-ISG在角膜表面滞留时间得到延长,具有良好的角膜铺展效果。同时其眼部生理相容性良好,无刺激性。结论:TMC包衣的VAPL-ISG具有阳离子脂质体和原位凝胶的优势,可延长角膜滞留时间,并具有良好的生物相容性,具备良好的应用开发前景。
OBJECTIVE: To study the corneal retention properties of ocular cationic liposomes coated with N-trimethyl chitosan (TMC) using vitamin A palmitate (VAP) as a model, Corneal irritation. METHODS: VAP liposome-in situ gels (VAPL-ISG) coated with TMC-coated VAPL-ISG were prepared by thin-film dispersion combined with ice-water bath stirring. Suspended vesicles and bound vesicles were used to study the kinetics of exfoliation on ex vivo eyeball surface. Draize score Law evaluation of corneal irritation in rabbits. Results: Transmission electron microscopy showed that VAPL-ISG had uniform particle size distribution and positive charge after coating. The TMC-coated VAPL-ISG has a longer corneal surface retention time compared to the nonapeptide gel and uncoated VAPL-ISG with good corneal spread. At the same time its eye physiologically compatible, non-irritating. CONCLUSION: TMC-coated VAPL-ISG possesses the advantages of cationic liposomes and in situ gels, prolongs corneal retention time, has good biocompatibility and possesses good application and development prospects.