维A酸隐形泡囊的制备及其体外性质的研究  

Preparation of Retinal acid stealth niosomes and evaluation of their characteristics in vitro

作　　者：卢进[1,2] 杨红[1] 牟家婉[3] 魏大鹏[3] 吴琼[1] 李雪[1] 程亚西[1] 莫生宁[1] 

机构地区：[1]四川大学华西药学院,四川成都610041 [2]广州合诚实业有限公司,广东广州410556 [3]四川大学华西基础与法医学院,四川成都610041

出　　处：《华西药学杂志》2009年第3期238-240,共3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：目的制备维A酸隐形泡囊并考察其理化、体外生物学性质。方法考察隐形泡囊的形态和粒径分布,经凝胶色谱分离,再用分光光度法测定维A酸的含量,计算包封率,测定冻干品的载药量;以普通泡囊的结果作为对照,考察巨噬细胞摄取率和癌细胞生长抑制率。结果维A酸泡囊和隐形泡囊的平均粒径分别为33、41μm,包封率分别为91.4%、93.10%,载药量分别为3.15%、2.82%。隐形泡囊规避巨噬细胞的吞噬能力提高26%以上;隐形泡囊与原药对癌细胞的生长抑制率相同。结论所制维A酸隐形泡囊的包封率高、操作方法简便;隐形泡囊既可保持较高抗癌活性,又能规避吞噬。OBJECTIVE To prepare Retinal acid stealth niosomes and evaluate their physicochemical and biological properties in vitro. METHODS The technology for preparation of stealth noisomes was optimized, and their morphology and particle sizes were evaluated. The entrapment efficiency （after separation by gel chromatography） and drug loading ratio of the lyophilized stealth niosomes were determined by UV spectrophotometry. The uptaken ratio of the stealth niosomes by MPM cells and the inhibition of carcinoma cell growth were studied as well, with the normal niosomes as the control. RESULTS The average sizes of the niosomes and the stealth niosomes were 33 and 41 um, respectively. The entrapment efficiencies, determined after separation by gel chromatography, were 91.4% and 93.1%, and drug loading ratios were 3.15 % and 2.82%, respectively. The uptaken ratio of the stealth niosomes by MPM cells decreased more than 26% , and the inhibition rate of carcinoma cell growth was the same as the ordinary drug. CONCLU- SION The Retinal acid stealth niosomes with high entrapment efficiency were easy to prepare based on simple procedures and showed high antitumor efficiency with evasion of phagocytosis by MPM cells.

关 键 词：维A酸 隐形泡囊 理化性质 抗癌活性 规避吞噬 

分 类 号：R94[医药卫生—药剂学]