摘要
目的:制备两亲性壳聚糖N-辛基-N,O-羧甲基壳聚糖包覆紫杉醇脂质体(PTX-LP-OCC),并考察其理化性质及体外释放行为。方法:采用基于乙醇的前体脂质体法制备紫杉醇脂质体并以OCC包覆,并以普通脂质体(PTX-LP)为对照,测定其包封率、粒径大小、电位,观测其形态及稳定性,然后采用全体液平衡反向透析法研究体外释放行为。结果:紫杉醇脂质体包封率为89.5%,粒径为236.5 nm,Zeta电位为-31.4 mV,多糖包覆修饰后药物包封率无显著变化,粒径及Zeta电位显著增加,脂质体稳定性显著提高,药物释放呈缓释特征,且突释显著降低。
Objective： To prepare paclitaxel loaded liposomes modified with amphiphilic chitosan deirvatives （N-octyl-N,O-carboxymethyl chitosan, OCC）, and investigate their characteristics and release behavior in vitro. Methods： Paclitaxel loaded liposomes modified with or without OCC （PTX-LP, PTX-LP-OCC） were prepared using an ethanol-based proliposome technology. Particle size and zeta potential of the liposomes were determined with Zetasizer 3000 HSa. The morphology was observed by a transmission electron microscope （TEM） technology. Stability of liposomes was evaluated by determining the particle size and drug leakage from liposomes. Finally, the in vitro release profiles of paclitaxel from PTX-LP and PTX-LP-OCC were evaluated using the bulk-equilibrium reverse dialysis bag technique. Results： Paclitaxel loaded liposomes were successfully prepared with an average diameter of 236.5 nm and zeta potential of -31.4 mV. The encapsulation efficiency was 89.5%. After OCC modification, there was no significant change in encapsulation efficiency, but the particle size and zeta potential significantly increased. As compared to PTX-LP, PTX-LP-OCC possessed better stability and lower burst release. Conclusion： Liposome modified with amphiphilic chitosan derivatives is a promising carrier for anticancer drug delivery.
出处
《药学与临床研究》
2012年第6期490-494,共5页
Pharmaceutical and Clinical Research
