摘要
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 prepare ocular cationic liposome-in situ gels coated by N-trimethyl chitosan （TMC） with vitamin A palmitate（VAP）as the model drug, and investigate their corneal retention and irritation behavior. METHODS The system （VAPL-ISG） was prepared by the film dispersion method combined with stirring in ice-water bath. The in vitro corneal retention behavior was evaluated by sessile bubble technique and captive bubble technique. Ocular irritation test was performed based on the Draize method. RESULTS Images of TEM showed that VAPL-ISG was uniformly distributed. The system presented electropositivity after TMC coating. The TMC coated VAPL-ISG exhibited longer corneal retention time and better wettability compared with Oculotect Gel and VAPL-ISG without TMC-eoating, while showed promising ocular eompatihility. CONCLUSION VAPL-ISG had both the advantages of cationic liposome and in situ gel after TMC coating. It could extend the corneal retention time with good ocular compatibility. The system was valuable to be studied further.
出处
《中国医院药学杂志》
CAS
CSCD
北大核心
2010年第19期1641-1644,共4页
Chinese Journal of Hospital Pharmacy
