多西紫杉醇脂质体的制备及稳定性考察

目的:制备多西紫杉醇脂质体并对其稳定性进行考察。方法:采用薄膜-超声分散法制备脂质体,利用高效液相色谱法测定其主药含量,并考察其粒径、Zeta电位、包封率等指标及在室温条件下密封放置2wk与4℃下冰箱中保存6mo的稳定性。结果:所得脂质体粒径小而均匀,粒径均值为(138.8±1.1)nm,Zeta电位为(2.25±0.2)mV,包封率均在70%以上;多西紫杉醇检测浓度线性范围为0.0325～2.600mg·mL-1(r=0.9993);平均回收率为100.91%(RSD=1.38%,n=3);稳定性考察各项指标均无明显改变。结论:所制制剂包封率较高,稳定性良好。

Preparation of Docetaxel Liposome and Investigation on Its Stability

OBJECTIVE: To prepare docetaxel liposome and to investigate its stability. METHODS: Docetaxel liposome was prepared with thin- film ultrasonic dispersion technology; the content of the principal agent was determined by HPLC; the indices such as grain size, Zeta potential, encapsulation efficiency, and its stability under the airtight storage for 2 weeks or stored at 4℃ for 6 months were investigated. RESULTS: The prepared liposome was small in grain size and well- distributed. The grain size, Zeta potential, and encapsulation efficiency of liposome were( 138. 8± 1. 1) nm, ( 2. 25± 0. 2) mV and above 70% , respectively. The linear range of docetaxel was 0. 032 5～ 2. 600mg· mL- 1( r=0. 999 3) , with average recovery at 100. 91% ( RSD=1. 38% , n=3) . No obvious changes were found in all the indices in the the stability of the liposome. CONCLUSION: The preparation was proved to be of high encapsulation efficiency and good stability.