紫杉醇长循环热敏前体脂质体的制备与表征

Preparation and Characteristics of Paclitaxel Long-circulating Thermo-sensitive Proliposomes

目的:研究紫杉醇长循环热敏前体脂质体的制备并对其性质进行考察。方法:采用薄膜分散法制备紫杉醇长循环热敏脂质体,再用冷冻干燥技术制备紫杉醇长循环热敏前体脂质体;采用激光粒度仪考察粒径和Zeta电位;采用高效液相色谱法研究其含量与包封率;并考察脂质体的体外释药特性。结果:紫杉醇长循环热敏前体脂质体水合后形成紫杉醇长循环热敏脂质体,粒径均值为(108.6±3.6)nm,Zeta电位的均值为(-12.2±1.8)mV,包封率可达96.2%;该脂质体在相变温度42℃下药物释放达到95%以上。结论:紫杉醇长循环热敏前体脂质体的制备工艺稳定,载药量大,包封率高,具有良好的热敏性;含量及其包封率测定方法简单、快速、准确。本实验可为紫杉醇静脉注射用新制剂的开发提供研究基础。

Objective：Preparation and characteristic of paclitaxel long- circulating thermo- sensitive proliposomes are studied. Methods： Paelitaxel long - circulating thermo - sensitive liposomes by film dispersion method vacuum freeze - drying technique was selected to dry pachtaxel long - circulating thermo - sensitive proliposomes, Its shape and size distribution were detected by transmission electron Zetasizer, and the content of paclitaxel was determined by HPLC, The encapsulation efficien- cy（EE） and the release rate of liposome were computed as well. Results：The mean encapsulation efficiency of the paclitaxel long - circulating thermo - sensitive proliposomes was （92. 6 ± 1.8 ） %, the appearance of liposomes was whole round, distribu- tion uniform,the mean particle size were（ 108.6 ±3. 6）nm,and zeta potential were（ - 12.2±1.8） mV. The liposome 42 ~C temperature under the drug release above 95%. Concluslon：The preparation technology of paclitaxel long - circulating thermo -sensitive proliposomes was stable, drug loading and entrapping capacity of liposomes were well. The methods for determination of paelitaxel content and entrapment efficiency were simple, rapid and accurate. These studies can provide bases for further development of intravenous injection paclitaxel thermo - sensitive liposomes.