Li R, Zhang Q, Wang X-y, Chen X-g, He Y-x, Yang W-y, Yang X
Key Laboratory of Food Biotechnology of Sichuan Province, School of Bioengineering, Xihua University, Chengdu, P. R. China.
West China School of Pharmacy, Sichuan University, Chengdu, P. R. China.
Drug Res (Stuttg). 2014 Oct;64(10):541-7. doi: 10.1055/s-0033-1363957. Epub 2014 Jan 17.
The transferring modified lipid coated PLGA nanoparticles, as a targetable vector, were developed for the targeting delivery of anticancer drugs with paclitaxel (PTX) as a model drug to the ovarian carcinoma, which combines the advantages and avoids disadvantages of polymeric nanoparticles and liposomes in drug delivery. A transmission electron microscopy (TEM) confirmed the lipid coating on the polymeric core. Physicochemical characterizations of TFLPs, such as particle size, zeta potential, morphology, encapsulation efficiency, and in vitro PTX release, were also evaluated. In the cellular uptake study, the TFLPs were more efficiently endocytosed by the A2780 cells with high expression of transferrin receptors than HUVEC cells without the transferrin receptors. Furthermore, the anticancer efficacy of TFLPs on the tumor spheroids was stronger than that of lipid coated PLGA nanoparticles (LPs) and PLGA nanoparticles. In the in vivo study, the TFLPs showed the best inhibition effect of the tumor growth for the ovarian carcinoma-bearing mice. In brief, the TFLPs were proved to be an efficient targeting drug delivery system for ovarian carcinoma.
以紫杉醇(PTX)为模型药物,开发了转铁蛋白修饰的脂质包衣聚乳酸-羟基乙酸共聚物纳米粒(TFLPs)作为靶向载体,用于将抗癌药物靶向递送至卵巢癌,该纳米粒结合了聚合物纳米粒和脂质体在药物递送方面的优缺点。透射电子显微镜(TEM)证实了聚合物核上的脂质包衣。还评估了TFLPs的物理化学特性,如粒径、ζ电位、形态、包封率和体外PTX释放。在细胞摄取研究中,与没有转铁蛋白受体的人脐静脉内皮细胞(HUVEC)相比,转铁蛋白受体高表达的A2780细胞更有效地内吞TFLPs。此外,TFLPs对肿瘤球体的抗癌功效强于脂质包衣聚乳酸-羟基乙酸共聚物纳米粒(LPs)和聚乳酸-羟基乙酸共聚物纳米粒。在体内研究中,TFLPs对荷卵巢癌小鼠的肿瘤生长显示出最佳抑制效果。简而言之,TFLPs被证明是一种有效的卵巢癌靶向给药系统。