论文部分内容阅读
目的:制备眼用N-三甲基壳聚糖(TMC)包覆的司帕沙星(SL)纳米脂质体原位凝胶(ISG),并考察其体外释放度。方法:采用p H梯度法制备SL脂质体,经高压均质至纳米级,用TMC包衣。以胶凝温度为指标,优选ISG基质泊洛沙姆407的最佳浓度,采用冷法制备TMC包覆SL纳米脂质体ISG。对TMC包覆SL纳米脂质体ISG中脂质体的形态、粒径、Zeta电位及包封率进行考察;以TMC包覆SL纳米脂质体为对照,采用无膜溶出模型考察其体外释药特性。结果:泊洛沙姆407的最佳浓度为25%,在人工泪液中的胶凝温度为23.6℃,稀释后的胶凝温度为33.5℃。TMC包覆SL纳米脂质体ISG中脂质体形态圆整,平均粒径为(96.8±1.5)nm,Zeta电位为(46.2±1.4)m V,包封率为(76.6±2.4)%,与TMC包覆SL纳米脂质体相比无明显变化。TMC包覆SL纳米脂质体ISG药物释放和凝胶溶蚀均为符合零级动力学特征,且与TMC包覆SL纳米脂质体相比,缓释性更为显著。结论:TMC包覆SL纳米脂质体ISG胶凝温度理想,并可延缓药物释放。
OBJECTIVE: To prepare in situ gel (ISG) of sparfloxacin (SL) coated with N-trimethyl chitosan (TMC) for ophthalmic use and investigate its in vitro release. METHODS: SL liposomes were prepared by gradient p H, homogenized to nanoscale by high pressure and coated with TMC. Taking gelling temperature as an index, preferably the optimal concentration of ISG substrate poloxamer 407, cold-prepared TMC-coated SL nanoliposome ISG was prepared. The morphology, particle size, Zeta potential and entrapment efficiency of liposomes in TMC coated SL nanosomes were investigated. TMC-coated SL nanosomes were used as control, Drug properties. Results: The optimal concentration of Poloxamer 407 was 25%, the gelation temperature in artificial tears was 23.6 ℃ and the gelation temperature after dilution was 33.5 ℃. The liposomes in the TMC-coated SL nanosomes were round, the average particle size was (96.8 ± 1.5) nm, the Zeta potential was (46.2 ± 1.4) mV, the encapsulation efficiency was (76.6 ± 2.4)%, Compared with TMC-coated SL nanosomes, there was no significant change. TMC coated SL nanoliposome ISG drug release and gel dissolution are in line with the zero-order kinetic characteristics, and compared with TMC coated SL nanoliposomes, sustained-release more pronounced. Conclusion: TMC-encapsulated SL nanoliposomes have an ideal gelation temperature and delayed drug release.