肺靶向顺铂隐形泡囊的研制及其体外生物学性质  

Preparation of lung-targeting Cisplatin stealth niosomes and evaluation of their in vitro characteristics

作　　者：陈永[1] 任林[2] 尹华熙[1] 魏大鹏[3] 王玉珍[4] 杨红[1] 

机构地区：[1]四川大学华西药学院,四川成都610041 [2]四川大学华西医院,四川成都610041 [3]四川大学华西基础医学院,四川成都610041 [4]四川大学化学学院,四川成都610064

出　　处：《华西药学杂志》2009年第1期1-5,共5页West China Journal of Pharmaceutical Sciences

基　　金：国家自然科学基金资助项目(批准号:30572262)

摘　　要：目的研制具有肺部靶向作用的隐形泡囊并进行体外抗癌细胞的实验评价。方法将亲水聚合物与胆固醇相连,考察含不同种类亲水链及含不同密度亲水链的隐形泡囊的包封率、稳定性和巨噬细胞吞噬作用,以最佳泡囊处方进行癌细胞生长抑制实验。结果用PluronicF68合成的胆固醇结合物所制隐形泡囊的包封率和固有水化层厚度较高,粒径合适;当胆固醇/Chol-PluronicF68的重量比为1:2.52时,泡囊的包封率、稳定性和体外规避巨噬细胞摄取等均较好,并具有和顺铂相似的抑制癌细胞生长的作用,粒径平均为8.432±0.043μm,有71.30%以上在被动肺靶向要求的7～25μm范围内,抑制癌细胞生长的结果与原料药顺铂相同。结论隐形泡囊制备简单,具有一定的隐形效果,能保持原药的抗癌活性,粒径范围符合被动肺靶向的要求。OBJECTIVE To prepare lung - targeting Cisplatin stealth niosomes and evaluate their antitumor efficiency in vitro. METHODS Several hydrophilic polymers were conjugated with cholesterol. Stealth niosomes with different kinds of hydrophilic poly- mers and with different density of hydrophilic chains were investigated in terms of entrapment efficiency, stability and phagocytosis test to choose the best formulation for antitumor experiments. RESULTS Stealth niosomes containing Pluronic F68 were chosen based on encapsulation efficiency, fixed aqueous layer thickness and suitable particle size. Stealth niosomes with a weight ratio of 1 ： 2.52 of cholesterol/high cholerterol - PluronicF68 were chosen for the subsequent experiments because of their high entrapment efficiency, sta- bility and low uptaken percentage in vitro. The mean size of particles was 8. 432 ± 0. 043 μm with 71.30% of the total hiosomes in the range of 7 - 25μm, which met the requirement of lung - targeting. Antitumor efficiency of the stealth niosomes was similar to Cisplatin solution. CONCLUSION The preparation method of stealth niosomes was simple and convenient. The stealth niosomes could maintain the antitumor activity of the drug and evade phagocytosis. The particle size range can meet the challenge of lung - targeting.

关 键 词：肺靶向 隐形泡囊 顺铂 吞噬 抗癌活性 

分 类 号：R94[医药卫生—药剂学]