文献：PLGA–LECITHIN–PEG CORE-SHELL NANOPARTICLES FOR CANCER TARGETED THERAPY

文献链接：https://www.worldscientific.com/doi/abs/10.1142/S1793984411000359

作者：MINGBIN ZHENG, PING GONG, DONGXUE JIA, CUIFANG ZHENG, YIFAN MA, and LINTAO CAI

We reported the development of multifunctional poly (lactic-co-glycolic acid) (PLGA)-lecithin-polyethylene glycol (PEG) core-shell nanoparticles (NPs) that combined the beneficial properties of liposome and polymeric NPs for chemotherapeutics delivery. The particle size, surface charge and surface functional groups were easily tunable in highly reproducible manner by various formulation parameters such as lipid/polymer, 1, 2-distearoyl-sn-glycero-3-phosphoethanolamine (DSPE)-PEG-COOH/lecithin, DSPE-PEG-COOH/DSPE-PEG-NH2 mass ratio and modification of terminal groups of DSPE-PEG. We encapsulated model chemotherapy drug, hydrophilic cisplatin (DDP) or hydrophobic DDP prodrug, in the NPs and showed high encapsulation efficiency, excellent stability, specific FA targeting recognition for MCF-7 cells with over FA receptors expression and pretty cytotoxicity. Such PLGA–lecithin–PEG core-shell nanoparticles (NPs) were proved to be a promising drug delivery nanocarrier for cancer-targeted therapy.

多功能聚乳酸-羟基乙酸共聚物（PLGA）-卵磷脂-聚乙二醇（PEG）核壳纳米粒子（NP）的开发，该纳米粒子结合了脂质体和聚合物NP的有益特性，用于药物的输送。

通过各种配方参数，如脂质/聚合物、1,2-二硬脂酰基-sn-甘油-3-磷酸乙醇胺（DSPE）-PEG-COH/卵磷脂、DSPE-PEG-COOH/DSPE-PEG-NH2质量比和DSPE-PEG末端基团的修饰，粒径、表面电荷和表面官能团很容易以高度可重复的方式进行调节。

我们将模型化疗药物亲水性顺铂（DDP）或疏水性DDP前药封装在NP中，并显示出高封装效率、优异的稳定性、对MCF-7细胞的特异性FA靶向识别，具有过FA受体表达和相当的细胞毒性。这种PLGA–卵磷脂–PEG核壳纳米粒子（NP）被证明是一种很有前途的癌症靶向治疗药物递送纳米载体。

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DSPE-PEG-Cy7

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DOPE-PEG-cRGD

DPPE-PEG-RGD

DMPE-PEG-RGD

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4-Arm PEG-DSPE

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