紫杉醇表面修饰脂质纳米粒的制备和性质  

Preparation and characterization of long-circulating solid lipid nanoparticles containing paclitaxel

作　　者：陈大兵[1] 吕万良[1] 杨天智[1] 李静 张强[1] 

机构地区：[1]北京大学药学院药剂学系,北京100083

出　　处：《北京大学学报（医学版）》2002年第1期57-60,共4页Journal of Peking University:Health Sciences

基　　金：国家自然科学基金 ( 39870 897)资助~~

摘　　要：目的 :以硬脂酸为载体材料制备紫杉醇的长循环脂质纳米粒。方法 :用“乳化蒸发 低温固化”法制备纳米粒 ;用透射电镜考察了纳米粒的形态 ;建立了于脂质纳米粒和血清中测定紫杉醇的HPLC方法 ;考察了纳米粒于30 % (体积分数 )乙醇溶液中的药物释放 ;以市售紫杉醇注射剂和自制的紫杉醇普通纳米粒为对照 ,测定了长循环纳米粒于小鼠体内的药物动力学参数。结果 :紫杉醇长循环脂质纳米粒的体内半衰期为 1 0 .1h ,同时普通纳米粒的体内半衰期为 2 .3h ,注射剂的体内半衰期为 1 .3h。结论 :长循环脂质纳米粒可以延长紫杉醇的体内半衰期。Objective: To prepare long circulating solid lipid nanoparticles containing paclitaxel with stearic acid. Methods: The stearic acid solid lipid nanoparticles containing paclitaxel were prepared by the method of 'emulsion evaporation solidification at low temperature'. Its morphology was examined by transmission electron microscope. The HPLC method for determination of paclitaxel in nanoparticles or blood samples was established. The release of paclitaxel in vitro and the pharmacokinetics after iv bolus injection to mice were studied. Results: Long circulating nanoparticles containing paclitaxel had a mean diameter of 220 nm. Long circulation nanoparticles could stay in the blood circulation for a longer time, with an increased T 1/2β 10.1 h , against T 1/2β 2.3 h of conventional nanoparticles and T 1/2β 1.3 h of paclitaxel injection. Conclusion: The long circulating nanoparticles can pronouncedly increase the circulation time of paclitaxel in blood stream.

关 键 词：长循环纳米粒 紫杉醇 药代动力学 药物载体 抗癌药 脂质纳米粒 制备 性质 

分 类 号：R979.1[医药卫生—药品] R966[医药卫生—药学]