两亲性壳聚糖包覆紫杉醇脂质体的制备及体外释放研究

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。结论:两亲性壳聚糖包覆脂质体是一个有前景的抗肿瘤药物递送载体

Preparation and in vitro Release of Paclitaxel Loaded Liposomes Modified with Amphiphilic Chitosan Derivatives

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.