RGD修饰共载紫杉醇和Rg3脂质体的制备及其体外评价

Preparation and properties of RGD modified paclitaxel and Rg3 loaded liposome in vitro

目的采用薄膜分散法制备精氨酸-甘氨酸-天冬氨酸(RGD)修饰共载紫杉醇(PTX)和抗新生血管药物Rg3的脂质体(RGD-LP-PTX/Rg3),评价其体外性质。方法采用薄膜分散法制备RGD修饰共载PTX和Rg3的脂质体,考察其形态、粒径、电位、包封率以及体外稳定性;通过MTT实验考察脂质体对HepG2、HUVEC细胞的毒性;通过HepG2、HUVEC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RGD-LP-PTX/Rg3的平均粒径为106.8±11.5 nm,Zeta电位为-3.50±2.83 mV,24 h内具有良好的血清稳定性。RGD-LP-PTX/Rg3的细胞毒性优于各对照组。体外细胞摄取实验表明:RGD-LP摄取HepG2细胞的效率是LP的2.6倍。RGD-LP摄取HUVEC细胞的效率是LP的3.5倍。结论 RGDLP-PTX/Rg3的制备工艺简单,与肿瘤细胞具有良好的亲和性,是一种高效的肿瘤靶向和新生血管靶向给药系统。

OBJECTIVE To prepare RGD conjugated paclitaxel（FFX） and Rg3 loaded liposome and evaluate their physicochemical properties and in vitro. METHODS The liposomes were prepared by thin film hydration method. The appearance, particle size,Zeta potential,encapsulation efficiency and in vitro stability of the liposomes in serum were evaluated. Cytotoxicity to HepG2, HUVEC of liposome was determined by MTT method. RESULTS The particle diameter of the liposome was 106.8 ± 11.5 nm with Zeta potential of - 3.50±2.83 mV. The result demonstrated that the RGD - LP - PTX/Rg3 uptaken by HepG2 were 2.6 times higher than that of the liposomes without RGD. RGD - LP uptaken by HUVEC were 3.5 folder higher than that of liposome. CONCLUSION RGD - LP - PTX/Rg3 is easy to prepare and a potential delivery system for tumor and neovascular targeting.