薄膜分散法制备白藜芦醇长循环热敏前体脂质体及其表征研究

Preparation and Characteristics of Resveratrol Long-Circulating Thermo-Sensitive Proliposomes

目的:对白藜芦醇长循环热敏前体脂质体制备的研究以及对其性质进行分析。方法:先用薄膜分散法制备白藜芦醇长循环热敏脂质体后,再用冷冻干燥法来制备白藜芦醇长循环热敏脂质体的前体。采用电势测定仪、HPLC等方法对该脂质体的包封率、粒径、稳定性、载药量、电位、释放度等来展开系统的检查。结果:白藜芦醇长循环热敏前体脂质体水合后形成白藜芦醇长循环热敏脂质体,粒径均值为(107.9±3.6)nm,Zeta电位的均值为(-12.2±1.6)m V,包封率可达89.4%;该脂质体在相变温度42℃下药物释放达到94%以上。结论:采用长循环热敏来制备的白藜芦醇前体脂质体含量与包封率检查方法准确、快速、简单且方法简便易行。载药量大,包封率好,工艺比较稳定。本实验可为新型白藜芦醇静脉注射用热敏脂质体的研究提供基础。

Objective： Preparation and characteristic of resveratrol long-circulating thermo-sensitive proliposomes are studied.Methods： resveratrol long-circulating thermo-sensitive liposomes by film dispersion method vacuum freeze-drying technique was selected to dry etoposide long-circulating proliposomes, Its shape and size distribution were detected by transmission electron Zetasizer,and the content of resveratrol was determined by HPLC, The encapsulation efficiency（ EE） and the release rate of liposome were computed as well. Results：The mean encapsulation efficiency of the etoposide long-circulating proliposomes was 89.4% the appearance of liposomes was whole round, distribution uniform, the mean particle size were（107.9±3.6）nm nm, and zeta potential were（-12.2±1.6）m V. The liposome 42 ℃ temperature under the drug release above 94%. Conclusion：The methods for determination of resveratrol content and entrapment efficiency were simple, rapid and accurate. These studies can provide bases for further development of intravenous injection resveratrol thermo-sensitive liposomes.The preparation technology of resveratrol long-circulating thermo-sensitive proliposomes was stable, drug loading and entrapping capacity of liposomes were well.