T7/A7R肽修饰的替莫唑胺脂质体制备与表征  

Preparation and Characterization of Temozolomide Liposomes Modified with T7/A7R Peptides

作　　者：林雯[1] 廖翔茹 史琼枝 李银科 谢向阳 胡华 Lin Wen;Liao Xiangru;Shi Qiongzhi;Li Yinke;Xie Xiangyang;Hu Hua(Department of Clinical Laboratory,Huangshi Love and Health Hospital,Hubei Huangshi 435000,China;Department of Pharmacy,General Hospital of Central Theater Command of the PLA)

机构地区：[1]黄石市爱康医院检验科,湖北黄石435000 [2]中国人民解放军中部战区总医院药剂科

出　　处：《中国药师》2021年第11期1978-1982,共5页China Pharmacist

基　　金：湖北省卫生健康科研基金项目(编号:WJ2019H422,WJ2021M218);湖北省自然科学基金项目(编号:2020CFB569);武汉中青年医学骨干人才培养工程(第六批)。

摘　　要：目的:制备由T7、A7R肽双重修饰的替莫唑胺脂质体,并进行初步的体外表征。方法:分别将T7、A7R与DSPE-PEG_(2000)-Mal反应生成DSPE-PEG_(2000)-T7和DSPE-PEG_(2000)-A7R,逆相蒸发法制备双肽修饰的脂质体(T7/A7R-LP),并进行相应的体外表征。结果:制备的脂质体近球形,粒径均匀,平均粒径(96.6±6.5)nm,zeta电位为-(5.15±1.03)mV,包封率(36.38±3.95)%;在4~8℃条件下放置30 d,粒径和zeta电位无显著变化,体外6 h释药完毕;细胞摄取试验表明T7/A7R-LP具有较好的脑部靶向递送能力。结论:制备的T7/A7R肽修饰的脂质体理化特性良好,性质较为稳定,具有一定的脑部药物递送前景。Objective:To prepare and evaluate temozolomide liposomes modified by T7 and A7 R peptides.Methods:T7 and A7 R peptides were mixed with DSPE-PEG-MALs to synthesize DSPE-PEG_(2000)-T7 and DSPE-PEG_(2000)-A7 R,respectively.And then the peptide modified liposomes(T7/A7 R-LP)loaded temozolomide were prepared by a reverse phase evaporation method,and the characteristics of T7/A7 R-LPs were assayed by transmission electron microscope,laser light scattering granularity instrument and so on.Results:The prepared T7/A7 R-LPs were round and uniform with the mean particle size of(96.6±6.5)nm,zeta potential of[-(5.15±1.03)]mV and drug entrapment efficiency of(36.38±3.95)%.T7/A7 R-LPs were stable during the incubation at(4-8)℃for 30 d and the drug could be completely released within 6 h.Conclusion:The prepared liposomes have good characteristics to be a potential vehicle for the brain targeting delivery of drugs.

关 键 词：多肽 脂质体 替莫唑胺 脑靶向 

分 类 号：R944.9[医药卫生—药剂学]