黄芩素长循环脂质体处方优化研究

Study on Optimizing Prescription of Baicalein Long Circulating Liposomes

目的:研究黄芩素长循环脂质体的处方优化。方法:采用逆相蒸发法制备脂质体。以HPLC法测定脂质体中黄芩素的含量,计算包封率和载药量,采用单因素和正交试验法优化黄芩素长循环的处方。结果:制备黄芩素长循环脂质体最佳处方为胆固醇与卵磷脂的比例为1∶2,处方中PEG4 000的量为2 mg,水相与有机相的比例取1∶2,黄芩素质量为30 mg。结论:经处方优化后,制备的黄芩素长循环脂质体平均包封率为81.42%,平均载药量为32.25%。

Objective： To optimize the prescription of baicalein long circulating liposomes（Baicalein LCLs）.Methods：The liposomes were prepared by the reverse evaporating method.The entrapment efficiency and the carrying amount were determined by HPLC-Sephadex method.The main influencing factors were identified by single factor analysis,then the techniques of the prescription and preparation of liposomes were optimized by orthogonal experiment.Results： The best prescription was as follows： The proportionality of cholesterin to lecithin was 1∶2;The dosage of PEG 4 000 was 2 mg;The proportionality of water phase to oil phase was 1∶2;The dosage of baicalein was 30 mg.Conclusion： After optimized,the average entrapment efficiency of liposomes is 81.42% and the average carrying amount is 32.25%.