注射用姜黄素脂质体的制备及其质量评价

Preparation and Quality Evaluation of Curcumin Liposome for Injection

目的:制备载药量高、包封率高、粒径均匀、稳定性好的注射用姜黄素脂质体,并对其质量进行评价。方法:采用薄膜分散高压均质法结合冻干工艺制备;考察脂质体的形态、粒径分布、zeta电位,用超滤离心法测定脂质体的包封率;通过加速稳定性实验对脂质体的稳定性进行考察;以自制的姜黄素注射液为参比制剂,比较了对小鼠肝癌瘤株H22和肺癌瘤株Lewis的抑制作用。结果:复溶后,姜黄素脂质体的平均粒径为120.1nm,zeta电位-50.5mV,包封率(95.45±0.86)%,载药量(4.1±0.1)%,加速试验中各项指标未发生明显变化,与姜黄素注射液相比,姜黄素脂质体对小鼠肝癌瘤株H22的抑瘤率可增加31.5%(P<0.01),对小鼠肺癌瘤株Lewis的抑瘤率可增加22.9%(P<0.01)。结论:姜黄素制成脂质体后,能提高稳定性,抑瘤率有显著的提高。

AIM： To prepare and evaluate the quality of curcumin liposomes , which were high drug load, high entrapment efficiency and good stability. METHODS： Curcumin liposomes were prepared by thin film-dispersion high pressure homogenization. The shape of liposomes , particles size, zeta potential and stability were evaluated. Entrapment efficiency and drug loading were determined by centrifugal ultrafiltration. RESULTS： The average diameter and zeta potential of curcumin liposomes were 120.1 nm and - 50.5 mV. The entrapment efficiency was （95.45 ± 0.86） % and drug loading was （4.1 ± 0.1 ） %. The antiumor activity of curcumin liposomes increased 31.5% in H22 cells, and 22.9% in lewis tumor model, as compared to that of curcumin injection. CONCLUSION： The incorporation of curcumin into liposomes can increase the curcumin stability and antitumor activity.