以商业化的端羧基聚乳酸-羟基乙酸共聚物(PLGA-COOH)和氦基聚乙二醇羧基(NH_2-PEG-COOH)为原料,以生物型分子1-(3-二甲氦基丙基)-3-乙基碳二亚胺盐酸盐(EDC)和N-羟基琥珀酰亚胺(NHS)为媒介,以4-二甲氦基吡啶(DMAP)为催化剂,通过简单、绿色的羧基和胺基的偶联反应,制备了聚乳酸羟基乙酸/聚乙二醇(PLGA-PEG)共聚物分子,并以该PLGA-PEG分子为载体包裹色素上皮衍生因子(PEDF),得到了PLGA-PEG/PEDF乳剂,并进一步考察了该乳剂作为抑制血管内皮生长因子(VEGF)的潜能.采用核磁共振氢谱表征了PLGA-PEG分子结构及其接枝率,并进一步表征了在不同条件下,PLGA-PEG/PEDF乳剂对人脐静脉内皮细胞(HUVEC)中VEGF水平的抑制作用.结果表明,以偶联法制备的PLGA-PEG分子为载体,得到的PLGA-PEG/PEDF乳剂具有良好的生物安全性,其对VEGF具有较高的抑制作用.
A biodegradable poly(lactic-co-glycolic acid)/polyethylene glycol (PLGA-PEG) copolymer molecule was prepared by the simple and green coupling reaction between carboxyl group of poly(lactide-co-glycolide)-carboxylic acid endcap (PLGA-COOH) and amino group of poly(ethylene glycol)amine and carboxylic acid endcap (NH2-PEG-COOH) in the presence of 1-ethyl-3-[3-dimethylaminopropyl]carbodiimide hydrochloride (EDC) and N-hydroxysuccinimide (NHS). The molecular structure of PLGA-PEG copolymer was characterized by 1H NMR spectroscopy, and the grafting yield of polyethylene glycol (PEG) on poly(lactic-co-glycolic acid) (PLGA) was calculated. Furthermore, pigment epithelium-derived factor (PEDF) was encapsulated in the PLGA-PEG copolymer to prepare a PLGA-PEG/PEDF emulsion for highly efficient inhibition on vascular endothelial growth gene expression (VEGF). The results showed that the obtained PLGA-PEG copolymer was bio-safety and the PLGA-PEG/PEDF emulsion was a good agent for effective inhibition VEGF expression under different conditions. Thus, the PLGA-PEG copolymer can be used as a bio-carrier and the PLGA-PEG/PEDF emulsion can be used as a good angiogenesis inhibitor, which has a potential application for some diseases by anti angiogenesis.