摘要
目的以胰岛素(INS)为模型药物,制备眼用阳离子纳米脂质体-原位凝胶(ISG),并对其相关体外性质及体外释药行为进行考察。方法采用逆向蒸发法制备INS纳米脂质体(INSL),并用N-三甲基壳聚糖(TMC60)进行包衣;根据胶凝温度筛选出泊洛沙姆407的最佳质量浓度;采用无膜溶出模型考察凝胶的体外释药行为。结果 TMC60包衣前的INSL-ISG的平均粒径为(92.36±0.20)nm,Zeta电位为(-19.50±0.30)mV;TMC60包衣后的INSL-ISG的平均粒径为(93.93±0.19)nm,Zeta电位为(13.23±0.15)mV。泊洛沙姆407的最佳质量浓度为25%,经模拟泪液稀释前后的胶凝温度分别为23.9℃和34℃。TMC60-INSL-ISG的药物释放和凝胶溶蚀均呈现良好的零级释放特征。结论 TMC60-INSL-ISG兼有阳离子脂质体和原位凝胶的优势,延缓了药物的释放,为下一步探究提高其角膜滞留性奠定了基础。
Objective To prepare ocular insulin（INS）-loaded cationic nanoliposomes-in situ gels（ISG）and investigate their related characteristics and drug release profiles in vitro.Methods Insulin nanoliposomes（INSL） were prepared by the reverse evaporation method,then coated by N-trimethyl chitosan（TMC60）.The optimal amount of poloxamer407 was selected according to the gelation temperature.A novel membraneless model was used to study the drug release in vitro.Results The mean diameter of INSL-ISG before TMC60 coating was（92.36±0.20） nm with the Zeta potential of（-19.50±0.30） mV.The mean diameter of INSL-ISG after TMC60 coating was（93.93±0.19） nm with the Zeta potential of（13.23±0.15） mV.The optimal concentration of poloxamer407 in the formula was 25% with the gelation temperature of 23.9 ℃ and 34 ℃ before and after simulation tear dilution.Both the drug release in vitro and gel dissolution profiles of TMC60-INSL-ISG exhibited the characteristics of zero order kinetics.Conclusion TMC60-INSL-ISG showed the advantages of cationic liposomes and in situ gels,and could delay the drug release in vitro,which provided the basis for the further study on the cornea residence time promotion.
出处
《广东药学院学报》
CAS
2013年第1期1-5,共5页
Academic Journal of Guangdong College of Pharmacy
