利用DSPE-PEG-NH₂实现亲/疏水药物高效包载与靶向释放
参考文献:PLGA-卵磷脂-PEG核壳奈米离子适用于癌症复发靶点*联接://www.worldscientific.com/doi/abs/10.1142/S1793984411000359笔者:郑明斌, 网球, 贾冬雪, 郑翠芳, 马一帆, 和 蔡林涛节选:我简报一种多性能聚乳酸-乙酸乙酯酸共聚物 (PLGA)-卵磷脂-聚乙二醇 (PEG) 核壳微米再生顆粒剂 (NPs),该微米再生顆粒剂极具特征脂质体和配位混物微米再生顆粒剂的好处,能够用于递送放疗口服药治疗。该微米再生顆粒剂的孔径、界面带电粒子和界面官能团可在不同的配方内容因素更好改善,且从复高,假如脂质/配位混物、1,2-二硬脂酰-sn-甘油-3-磷酸乙酸乙酯胺 (DSPE)-PEG- COOH /卵磷脂、DSPE-PEG- COOH /DSPE-PEG- NH 2 的效果比及及 DSPE-PEG 端基的呈现。我将实体模型放疗口服药治疗——亲丙烯酸乳液顺铂 (DDP) 或疏丙烯酸乳液 DDP 前药——封装形式于微米顆粒剂 (NP) 中,没想到显现其包封率高、稳固性佳、对高 FA 蛋白激酶展现的 MCF-7 组织人体细胞极具特喜欢的人靶点分辨水平,且 FA 蛋白激酶展现量高,且组织人体细胞毒素较小。此种 PLGA-卵磷脂-PEG 核壳微米顆粒剂 (NP) 已被证明材料是一个种*具优势的肝癌靶点*口服药治疗递送微米质粒载体。AbstractWe 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.