pH敏感多肽修饰载紫杉醇脂质体的制备及评价

West China Journal of Pharmaceutical Sciences(2015)

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Abstract
目的 制备pH敏感多肽修饰载紫杉醇脂质体(pHS-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HepG2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pHS-LP-PTX在pH6.4时平均粒径为125.5 ±13.4 nm,Zeta电位为10.47±2.53 mV,24 h内具有良好的血清稳定性.MTT结果显示:pH6.4时,pHS-LP-PTX的细胞毒性优于各对照组.体外细胞摄取实验表明:pH6.4时,MCF-7细胞和HepG2细胞对pHS-LP-PTX的摄取效率优于pH7.4时和普通脂质体.结论 紫杉醇脂质体经过pH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pH敏感型肿瘤靶向给药系统.
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Key words
pH sensitive,Paclitaxel,Tumor targeting,Liposomes,Peptide modified,Thin film hydration method,Demonstrated
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