摘要
研究了齐墩果酸-乳酸羟基乙酸共聚物-水溶性维生素E-纳米粒(OA-PLGA-TPGS-NPs,即OA-NPs)在小鼠体内的分布及肝靶向性。按超声乳化-溶剂挥发法制备OA-NPs。经小鼠尾静脉给药,采用RP-HPLC法检测齐墩果酸在小鼠血浆、心、肝、脾、肺、肾中的浓度随时间的变化,与齐墩果酸溶液剂(OA-SOLs)组进行比较。OA-NPs组各时间点肝内药物浓度远高于OA-SOLs组,药物持续作用时间明显长于OA-SOLs组;OA-NPs组药物对肝的5个靶向指标值均显著高于OA-SOLs组;OA-NPs组各时间点血、心、肝、脾、肺、肾中药物浓度显著低于OA-SOLs组。OA-NPs可实现肝脏被动靶向,能够提高药物疗效,降低全身毒副作用。
The body distribution and hepatic targeting of oleanolic acid polylactic-co-glycolic acid D-ct-tocopherol polyethylene glycol 1 000 succinate nanoparticles (OA-PLGA-TPGS-NPs, OA-NPs) in mice was studied. OA-NPs were prepared by ultrasonic emulsification-solvent evaporation technique. The mice were given medicine by tail vein. Results show that intrahepatic drug concentration of OA-NPs is higher than that of OA-SOLs at different time points, and longer drug duration; the five targeted indexes of OA-NPs are higher than that of OA-SOLs; the concentrations in plasma,heart,liver, spleen,lung,kidney of OA-NPs are lower than that of OA-SOLs. So OA- NPs can realize the liver passively target, improve efficacy, and reduce systemic side effects
出处
《当代化工》
CAS
2013年第3期264-267,共4页
Contemporary Chemical Industry
关键词
齐墩果酸
纳米粒
体内分布
肝靶向
Oleanolic acid
Nanoparticles
Body distribution
Hepatic targeting