黄芩苷固体脂质纳米粒的制备及其在小鼠体内组织分布研究

目的制备黄芩苷固体脂质纳米粒(solid lipid nanoparticle,SLN),研究其在小鼠体内的组织分布并评价组织靶向性。方法采用乳化蒸发-低温固化法制备黄芩苷固体脂质纳米粒分散液,冷冻干燥成黄芩苷SLN冻干粉。灌胃给予黄芩苷-SLN干粉混悬液与黄芩苷混悬液,测定小鼠各组织中药物浓度,采用DAS 2.0软件拟合药物代谢动力学参数。计算靶向效率(targeting efficiency,Te)、靶向指数(targeting index,TI)和相对靶向效率(relative targeting efficiency,Rte),分析比较两种制剂在小鼠体内组织分布情况。结果小鼠灌胃黄芩苷-SLN冻干粉后,肝组织的Te最大;TI的大小顺序为脾、心、肝、脑、肾、肺,且仅脾、心的Rte为正值。结论黄芩苷-SLN肝组织分布量最大,脾组织靶向性较强,对黄芩苷临床应用具有重要意义。

Preparation of Baicalin Solid Lipid Nanoparticles and Its Tissue Distribution in Mice

Objective To prepare baicalin solid lipid nanoparticles (SLNs), and to investigate the tissue distribution of baicalin SLNs in mice and their tissue targeting ability. Methods Baicalin SLN dispersion liquid was prepared by the method of emulsification evaporation and low-temperature solidification and was then treated with freeze-drying technology to prepare the lyophilized powder of baicalin SLNs. The mice were given the suspension of the lyophilized powder of baicalin SLNs or baicalin suspension by gavage to determine the concentration of baicalin in various types of tissue, and DAS 2.0 pharmacokinetic software was used for the fitting of pharmacokinetic parameters. Targeting efficiency (Te), targeting index (TI), and relative targeting efficiency (Rte) were calculated, and the tissue distribution of these two preparations was compared. Results After the administration of the lyophilized powder of baicalin SLNs by gavage, the highest Te was observed in the liver tissue, the highest TI was observed in the spleen, followed by the heart, liver, brain, kidney, and lung, and positive Rte was observed only in the spleen and heart. Conclusion Baicalin SLNs are the most widely distributed in liver tissue and have a strong targeting ability for spleen tissue, which is of great significance to the clinical application of baicalin.