载RGD肽脂质体的优化和初步评价  

Optimization and Preliminary Evaluation of Liposomes Loaded with RGD Peptide

作　　者：王思明[1] 尹翌秋 张鹏飞[1] 孙天霞 齐滨[1] 

机构地区：[1]长春中医药大学中医药与生物工程研究开发中心,吉林长春130117 [2]长春金赛药业有限责任公司,吉林长春130012

出　　处：《中国医药工业杂志》2017年第5期706-710,共5页Chinese Journal of Pharmaceuticals

基　　金：吉林省中药生物技术重点实验室(20140622003JC);吉林省中药组学工程实验室(2014N155)

摘　　要：采用逆相蒸发法制备了载RGD肽脂质体。以包封率为指标,采用单因素试验和正交设计优化工艺条件。确定的优化条件为:卵磷脂和胆固醇的质量比为4∶1,磷酸盐缓冲液的体积为10 ml,RGD肽的加入量为18 mg,超声时间为3 min。3批优化制品平均粒径为473 nm,平均包封率为75.35%。RGD肽脂质体在磷酸盐缓冲液中16 h累积释放率为48.5%,相较于RGD肽溶液有一定的缓释效果。初步稳定性试验表明,载RGD肽脂质体在4℃保存相对较稳定。The purpose of the study is to investigate the factors influencing the preparation of RGD peptide liposomes. The optimum conditions were determined by orthogonal test. The properties of entrapment efficiency, stability and in vitro release were investigated. The RGD liposomes were prepared by reverse phase evaporation method. The formulation and process parameters of the liposomes were optimized by single factor test and orthogonal design with entrapment efficiency as the index. The optimal conditions were as follows： the mass ratio of lecithin to cholesterol was 4 ; 1, the volumn of phosphate buffer （PBS） was 10 ml, the amount of RGD （Arg-Gly-Asp） peptide was 18 mg and the ultrasound time was 3 min. The average diameter and entrapment efficiency of three batches of the optimal RGD peptide liposomes were 473 nm and 75.35 % . The cumulative release of RGD peptide from the liposomes at 16 h in PBS were 48.5 %, demonstrating certain sustained-release effect compared with the RGD peptide solution. The results of preliminary stability test showed that the RGD peptide liposomes stored at 4℃ were rather stable.

关 键 词：RGD肽 脂质体 逆相蒸发法 包封率 体外释放 稳定性 

分 类 号：R944.9[医药卫生—药剂学]