文献：Lipid-Polymer Nanoparticles for Folate-Receptor Targeting Delivery of Doxorubicin

作者：Zheng, Mingbin; Gong, Ping; Zheng, Cuifang; Zhao, Pengfei; Luo, Zhenyu; Ma, Yifan; Cai, Lintao

文献链接：https://www.ingentaconnect.com/contentone/asp/jnn/2015/00000015/00000007/art00004

摘要：

A biocompatible PLGA-lipid hybrid nanoparticles (NPs) was developed for targeted delivery of anticancer drugs with doxorubicin (DOX). The hydrodynamic diameter and zeta potential of DOX-loaded PLGA-lipid NPs (DNPs) were affected by the mass ratio of Lipid/PLGA or DSPE-PEG-COOH/Lecithin. At the 1:20 drug/polymer mass ratio, the mean hydrodynamic diameter of DNPs was the lowest (99.2±1.83 nm) and the NPs presented the encapsulation efficiency of DOX with 42.69±1.30%. Due to the folate-receptor mediated endocytosis, the PLGA-lipid NPs with folic acid (FA) targeting ligand showed significant higher uptake by folate-receptor-positive MCF-7 cells as compared to PLGA-lipid NPs without folate. Confocal microscopic observation and flow cytometry analysis also supported the enhanced cellular uptake of the FA-targeted NPs. The results indicated that the FA-targeted DNPs exhibited higher cytotoxicity in MCF-7 cells compared with non-targeted NPs. The lipid-polymer nanoparticles provide a solution of biocompatible nanocarrier for cancer targeting therapy.

开发了一种生物相容性PLGA-脂质杂化纳米粒子（NP），用于与阿霉素（DOX）靶向递送药物。

DOX负载的PLGA脂质NP（DNPs）的流体动力学直径和ζ电位受到脂质/PLGA或DSPE-PEG-COOH/卵磷脂质量比的影响。

在1:20的药物/聚合物质量比下，DNP的平均流体动力学直径低（99.2±1.83 nm），NP的DOX包封效率为42.69±1.30%。

由于叶酸受体介导的内吞作用，与不含叶酸的PLGA脂质NP相比，具有叶酸（FA）靶向配体的PLGA脂NP显示出叶酸受体阳性MCF-7细胞对叶酸的摄取明显更高。

共聚焦显微镜观察和流式细胞术分析也支持FA靶向NP的细胞摄取增强。

结果表明，与非靶向NP相比，FA靶向DNPs在MCF-7细胞中表现出更高的细胞毒性。脂质聚合物纳米颗粒为癌症靶向治疗提供了生物相容性纳米载体的解决方案。

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