甲基莲心碱纳米脂质体的研制及其体外释药特性考察

目的制备甲基莲心碱（Nef）纳米脂质体,并对其体外释药进行考察,为进一步体内研究奠定基础。方法采用薄膜分散法制备Nef脂质体,并乳匀至纳米级（NefNL）。以包封率为指标,筛选NefNL的最佳处方,并对其形态、粒径及体外释药性质进行考察。结果筛选出的最优处方为：卵磷脂∶胆固醇质量比为5∶1,药物∶类脂质量比为1∶25,药物质量浓度为0.4 mg/mL,水化介质为pH6.5磷酸盐缓冲液。最优处方制备的纳米脂质体的包封率平均为（73.6±2.3）%;平均粒径为（82.5±6.8）nm;体外释药具有明显的缓释特征,符合H iguch i方程：Q=-0.1855＋0.2910t1/2,r=0.986 2。结论 NefNL外形圆整均匀,达到纳米级,缓释效果明显,值得进一步开展体内研究。

Studies on the preparation and release of neferine nanoliposomes in vitro

Objective To prepare neferine（Nef） nanoliposomes and study on their release characteristics in vitro.Methods Neferine nanoliposomes（NefNL） were prepared by the film dispersion method followed with extruding to nanoliposomes.The encapsulation rate（ER） was chosen as index to achieve optimal formulation.The appearance,size and its distribution,release in vitro of the nanoliposomes were investigated.Results The optimal formulation of NefNL was as follows： the ratio of lecithin and cholesterol of 5∶1,ratio of Nef and lipids of 1∶25,the drug concentration of 0.4 mg/mL and the hydration solution of PBS with pH6.5.The ER of the optimal formulation of NefNL was（73.6±2.3）% with the mean size of（82.5±6.8）nm.The drug release in vitro had significant sustained property and was accorded with the Higuchi equation： Q=-0.1855＋0.2910t1/2,r=0.9862.Conclusion The NefNL with promising ER,nanometeric sizes and sustained drug release deserves further study in vivo.