论文部分内容阅读
目的:以黄芩素为模型药物,单硬脂酸甘油酯为药物载体,研制黄芩素固体脂质纳米粒(Ba-SLNs),对制剂的性质及体内药动学进行初步评价。方法:采用溶剂注入法制备Ba-SLNs,以包封率为考察指标,正交试验优化其处方并对其包封率、粒径、Zeta电位和体外释放等性质进行考察,同时采用SD大鼠进行体内药动学的评价。结果:Ba-SLNs外观呈淡黄色乳光溶液,透射电镜下为球状实体,平均粒径为(107.42±2.38)nm、PDI为(0.216±0.12)、Zeta电位为(-31.5±1.42)mV、包封率和载药量分别为(81.2±1.5)%和(7.16±0.14)%。体外释放表明6 h内Ba-SLNs溶液释放仅48.26%,在36 h累计释放达到80%,具有明显的缓释效果,X射线分析表明了药物以无定型状态分散在脂质载体中。大鼠口服黄芩素原料药和Ba-SLNs后,后者的口服生物利用度提高了近2倍。结论:成功研制了Ba-SLNs,提高了药物的生物利用度。
OBJECTIVE: Baicalein-based solid lipid nanoparticles (Ba-SLNs) were prepared with baicalein as model drug and glyceryl monostearate as drug carrier. The properties and in vivo pharmacokinetics of baicalein were evaluated. Methods: Ba-SLNs were prepared by solvent injection method. The entrapment efficiency was used as the index to investigate the encapsulation efficiency. The orthogonal test was used to optimize the formulation and the encapsulation efficiency, particle size, Zeta potential and in vitro release were investigated. Meanwhile, In vivo pharmacokinetic evaluation. Results: The appearance of Ba-SLNs was a light yellow opalescent solution. The average diameter of Ba-SLNs was (107.42 ± 2.38) nm, the PDI was (0.216 ± 0.12) and the zeta potential was (-31.5 ± 1.42) The encapsulation efficiency and drug loading were (81.2 ± 1.5)% and (7.16 ± 0.14)%, respectively. The release in vitro showed that the release of Ba-SLNs solution was only 48.26% within 6 h, and reached to 80% after 36 h. The X-ray analysis showed that the drug was dispersed in the lipid carrier in an amorphous state. After oral administration of Baicalein and Ba-SLNs, the oral bioavailability of the latter increased nearly two-fold. Conclusion: Ba-SLNs has been successfully developed to improve the bioavailability of drugs.