pH敏感多肽修饰载紫杉醇脂质体的制备及评价
Study on the preparation and properties of pH sensitive peptide modified paclitaxel loaded liposome in vitro
作者：龚锐;李胜英;黎云燕;
Author：
收稿日期： 年卷（期）页码：2015,30(02):-134-136
期刊名称：华西药学杂志
Journal Name：WEST CHINA JOURNAL OF PHARMACEUTICAL SCIENCES
关键字：pH敏感;紫杉醇;肿瘤靶向;脂质体;多肽修饰;薄膜分散法;细胞摄取
Key words：
基金项目：
中文摘要
目的制备p H敏感多肽修饰载紫杉醇脂质体(p HS-LP-PTX),并评价其体外性质。方法采用薄膜分散法制备PHS-LP-PTX,MTT实验考察脂质体对MCF-7细胞和Hep G2细胞的毒性,通过细胞摄取实验考察脂质体与肿瘤细胞的结合能力。结果所制备的p HS-LP-PTX在p H6.4时平均粒径为125.5±13.4 nm,Zeta电位为10.47±2.53 m V,24 h内具有良好的血清稳定性。MTT结果显示:p H6.4时,p HS-LP-PTX的细胞毒性优于各对照组。体外细胞摄取实验表明:p H6.4时,MCF-7细胞和Hep G2细胞对p HS-LP-PTX的摄取效率优于p H7.4时和普通脂质体。结论紫杉醇脂质体经过p H敏感多肽修饰后,能增强脂质体在酸性环境下的细胞穿透能力,是一种良好的p H敏感型肿瘤靶向给药系统。
参考文献
[1]Wojtkowiak JW.Drug resistance and cellular adaptation to tumor acidic p H microenvironment[J].Mol Pharm,2011,8(6):2032-2038.
[2]Zhang QY.A p H-responsive a-helical cell penetrating peptidemediated liposomal delivery system[J].Biomaterials,2013,34(32):7980-7993.
[3]Zhang W.Design of acid-activated cell penetrating peptide for delivery of active molecules into cancer cells[J].Bioconjug Chem,2011,22(7):1410-1415.
[4]Beata Chertok.Substantiating in vivo magnetic brain tumor targeting of cationic iron oxidenanocarriers via adsorptive surface masking[J].Biomaterials,2009,3(4):1-8.
[5]Yao Q.Liposome formulated with TAT-modified cholesterol for improving brain delivery and therapeuticefficacy on brain glioma in animals[J].Int J Pharm,2011,420(2):304-312.
[6]Yao Q.Liposome formulated with TAT-modified cholesterol for enhancing the brain delivery[J].Int J Pharm,2011,419(1):85-95.
[7]Chee WG.Transferrin-conjugated nanoparticles of poly(lactide)-D-a-tocopheryl polyethylene glycol succinate diblock copolymer for targeted drug delivery across the bloodbrain barrier[J].Biomaterials,2010,31(30):7748-7757.
[8]Ying X.Dual-targeting daunorubicin liposomes improve the therapeutic efficacy of brain glioma in animals[J].J Control Rel,2010,141(2):183-192.
[9]Garcia GE,Andrieux K,Gil S,et al.Colloidal carriers and blood brain barrier(BBB)translocation:A way to deliver drugs to the brain[J].Int J Pharm,2005,298:274-292.
[10]Zhan C,Gu B,Xie C.Cyclic RGD conjugated poly(ethyleneglycol)-co-poly(lactic acid)micelle enhances paclitaxel antiglioblastoma effect[J].J Control Rel,2010,143(1):136-142.
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