摘要
高密度脂蛋白(HDL)可逆向转运血浆中胆固醇至肝脏代谢,在肝靶向传递系统方面具有较大的开发潜力和、应用价值。载脂蛋白A-Ⅰ(apoA-Ⅰ)是HDL的主要组成部分。以apoA-Ⅰ为载体,水溶性抗肿瘤药盐酸多柔比星为模型药,采用薄膜分散法或硫酸铵梯度法制备重组高密度脂蛋白-盐酸多柔比星纳米粒,并以平均粒径或包封率为指标进行优化。结果表明,优化后的薄膜分散法所得制品平均粒径为(48.3±16.1)nm,包封率为(20.2±4.2)%。优化后的硫酸铵梯度法所得制品平均粒径为(113.8±10.3)nm,包封率为(83.3±8.5)%,且无溶血性。采用5%蔗糖为冻干保护剂制得的冻干,品于-20℃放置8个月,稳定性较好。
High density lipoprotein （HDL） can reverse transport cholesterol from plasma to liver, which has the considerable potential for development and application as a liver targeting delivery system. Apolipoprotein A- I （apo A- I ） is the major component of HDL. The reconstituted high density lipoprotein-drug nanoparticles were prepared by thin-film dispersion method or ammonium sulfate-gradient method with apo A- I as the carrier and water- soluble antineoplastic agent doxorubicin hydrochloride as the model drug. The two preparation methods were optimized with mean diameter or entrapment efficiency as the index. The mean diameter of optimal products prepared by thin- film dispersion method and ammonium sulfate-gradient method were （48.3±16.1）nm and （113.8±10.3）nm, with the entrapment efficiency of （20.2±4.2） % and （83.3±8.5） %, respectively. The product prepared by the latter method had no hemolysis in vitro and the lyophilized product with 5 % sucrose as the lyoprotectant stored at -20℃ for 8 months was fairly stable.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2012年第7期558-561,567,共5页
Chinese Journal of Pharmaceuticals
基金
国家自然科学基金(30973684)
上海市科委纳米专项资助(0952nm03500)
关键词
高密度脂蛋白
载脂蛋白A-Ⅰ
水溶性药物
盐酸多柔比星
肝靶向
制备
high density lipoprotein
apolipoprotein A- I
water-soluble drug
doxorubicin hydrochloride
livertargeting
preparation
