摘要
目的制备整合素受体精氨酸-甘氨酸-天冬氨酸(Arg-Gly-Asp,RGD)修饰共载紫杉醇和姜黄素脂质体(RGDLP-PTX/Cu),研究其卵巢癌细胞靶向性以及对卵巢癌的治疗效果。方法采用薄膜分散法制备RGD修饰共载紫杉醇和姜黄素脂质体(RGDLP-PTX/Cu)。观察脂质体的粒径,电位以及包封率;通过细胞摄取实验研究卵巢癌细胞(A2780)对普通脂质体(LP)和RGD修饰脂质体(RGDLP)的摄取效率。流式细胞仪检测不同载药脂质体诱导肿瘤细胞凋亡;构建卵巢癌裸鼠异位模型,考察不同载药脂质体对肿瘤生长抑制作用。结果 RGDLP-PTX/Cu的粒径在(94.8±11.2)nm,电位为(-3±2.45)mV,PTX与Cu的包封率分别为81.8%和84.6%。细胞摄取实验结果显示,A2780细胞对RGDLP的摄取效率是LP的3.6倍;凋亡实验表明RGDLP-PTX/Cu诱导卵巢癌细胞凋亡的能力显著强于RGDLP-PTX、RGDLP-Cu和LP-PTX/Cu(P<0.01);荷瘤裸鼠肿瘤生长抑制实验结果表明:RGDLP-PTX/Cu具有良好的抗卵巢癌作用(P<0.01)。结论 RGD修饰共载紫杉醇和姜黄素脂质体具有良好的卵巢癌细胞靶向性和抗卵巢癌作用,是一种潜在高效的卵巢癌靶向给药系统。
Objective To prepare RGD conjugated paclitaxel and curcumin loaded liposome and evaluate their properties and effect on the treatment of ovarian carcinoma in vitro and in vivo . Method The liposomes were prepared by thin film hydration method. The particle size,Zeta potential and entrapment efficiency were evaluated. The efficiency of cellular uptake on A 2780 cells in vitrowas evaluated. Flowcytometry were used to observe the apoptosis morphous.A 2780 cells werexenografted in athymic mice to establish the animal model, which were used to evaluate the effect of anti-cancer. Results The particle diameter of the RGDLP-PTX/Cu was (94.8±11.2) nm with the Zeta potential of (-3±2.45) mV. The entrapment efficiency of PTX and Gen were 81.8%and 84.6%respectively. The result demonstrated that RGDLP uptaken by A 2780 were 3.6 times higher than that of LP. The apoptosis assay、the inhibition of the inhibition of tumor in vivoconfirmed strong inhibitory effect ofRGDLP-PTX/Cu. Conclusion RGDLP-PTX/Cu were easy to prepare and it is a potential delivery system for the treatment of ovarian carcinoma.
出处
《中国生化药物杂志》
CAS
北大核心
2014年第1期62-64,共3页
Chinese Journal of Biochemical Pharmaceutics
