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。 RGD peptide liposomes were prepared by reverse phase evaporation. Using entrapment efficiency as an index, single factor experiments and orthogonal design were used to optimize the process conditions. The optimized conditions were as follows: the mass ratio of lecithin to cholesterol was 4:1, the volume of phosphate buffer solution was 10 ml, the amount of RGD peptide was 18 mg and the time of ultrasound was 3 min. The average particle size of 3 batches of optimized products was 473 nm with the average entrapment efficiency of 75.35%. The cumulative release rate of RGD peptide liposomes in phosphate buffered saline solution for 48 h was 48.5%, which showed a sustained release effect compared with RGD peptide solution. Preliminary stability tests showed that the RGD peptide-loaded liposomes were relatively stable at 4 ° C.