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目的制备黄芩苷类脂纳米囊(BA-LNC)并考察其理化性质和大鼠口服药物动力学。方法以中链甘油三酯(MCT)为油相,聚乙二醇单硬脂酸酯(Solutol HS15)为表面活性剂,卵磷脂为助乳化剂,采用相转化法制备类脂纳米囊(LNC),以包封率(EE)和载药量(DL)为指标,通过单纯形网格法对处方因素进行优化,采用响应面法对实验结果进行处理,得最优处方。采用Wistar大鼠研究BA-LNC制剂的口服药物动力学。结果制备的BA-LNC包封率为92.58%,载药量为1.69%。在透射电镜下BA-LNC呈类球形,分散良好,无粘连,平均粒径为(84.2±1.7)nm,多分散指数为0.201,Zeta电位为(-13.2±0.62)m V,制剂可显著延长药物在体内的滞留时间,增大其口服吸收。结论 BA-LNC可显著增大黄芩苷的口服生物利用度。
Objective To prepare baicalin lipid nanocapsules (BA-LNC) and study its physicochemical properties and oral pharmacokinetics in rats. Methods Liposome nanocapsules (LNCs) were prepared by a phase inversion method using medium-chain triglycerides (MCT) as the oil phase, Solutol HS15 as the surfactant and lecithin as the co-emulsifier ). The encapsulation efficiency (EE) and drug loading (DL) were used as indexes to optimize the prescription factors by the simplex grid method. The response surface method was used to process the experimental results to obtain the optimal prescription. Oral pharmacokinetics of BA-LNC formulations were studied using Wistar rats. Results The encapsulation efficiency of BA-LNC was 92.58% and the drug loading was 1.69%. BA-LNC showed a spheroidal shape with good dispersion and no adhesions under transmission electron microscopy. The average particle size was (84.2 ± 1.7) nm, the polydispersity index was 0.201 and the zeta potential was (-13.2 ± 0.62) mV. Drug residence time in the body, increasing its oral absorption. Conclusion BA-LNC can significantly increase the oral bioavailability of baicalin.