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Synthesis and characterization of pH sensitive Poly(PEGDMA-MAA) copolymeric microparticles for oral insulin delivery

机译:用于口服胰岛素递送的pH敏感型聚(PEGDMA-MAA)共聚微粒的合成与表征

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Poly(ethylene glycol) dimethacrylates (PEGDMA) were synthesized by esterification reaction of different molecular weight poly(ethylene glycol) with methacrylic acid in presence of acid catalyst. Their degrees of acrylation were found to be in the range of 93-95%, using nuclear magnetic resonance (NMR) spectroscopy. PEG dimethacrylates of molecular weight ranging from 400 to 4000 and methacrylic acid were further copolymerized to obtain pH sensitive crosslinked hydrogel microparticles. The diameters of poly(PEGDMAMAA) microparticles increased with increasing molecular weight of the poly(ethylene glycol) dimethacrylates and was found to be in the range of 0.4-2.7 mu m at pH 7.4 and 5.2-25.3 mu m at pH 2.5 in aqueous solution. Surface morphology of various polymeric samples were observed using SEM, which showed partial aggregation of particles at pH 2.5 but microparticles coalesce with each other and appeared like a continuous film at pH 7.4. In vitro insulin release studies were performed by simulating the condition of gastrointestinal tract, which showed only 18-25% insulin release into the aqueous medium at pH 2.5 in 90 min, while significantly higher release was observed at pH 7.4. In studies with diabetic rabbits, the blood glucose levels were lower for animals that received the insulin loaded hydrogel microparticles and the effect lasted for 8-10 h. (C) 2007 Wiley Periodicals, Inc.
机译:在酸催化剂的存在下,通过不同分子量的聚乙二醇与甲基丙烯酸的酯化反应合成了聚乙二醇二甲基丙烯酸酯(PEGDMA)。使用核磁共振(NMR)光谱发现它们的丙烯酸化程度在93-95%的范围内。将分子量为400至4000的PEG二甲基丙烯酸酯与甲基丙烯酸进一步共聚以获得pH敏感的交联水凝胶微粒。聚(PEGDMAMAA)微粒的直径随着聚(甲基)乙二醇二甲基丙烯酸酯的分子量的增加而增加,并且在水溶液中在pH 7.4下发现其直径在0.4-2.7μm和在pH 2.5下处于5.2-25.3μm。 。使用SEM观察到各种聚合物样品的表面形态,其在pH 2.5下显示出颗粒的部分聚集,但是微粒彼此聚结并且在pH 7.4下看起来像连续膜。通过模拟胃肠道状况进行了体外胰岛素释放研究,该实验表明在90分钟内pH值为2.5时只有18-25%的胰岛素释放到水性介质中,而在pH 7.4时则观察到明显更高的释放。在糖尿病兔子的研究中,接受胰岛素负载水凝胶微粒的动物的血糖水平较低,这种作用持续了8-10小时。 (C)2007 Wiley期刊公司

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