Design of poly(ethylene glycol)-tethered copolymers as novel mucoadhesive drug delivery systems
Design of poly(ethylene glycol)-tethered copolymers as novel mucoadhesive drug delivery systems
复制标题
DOI：
10.1016/j.ejpb.2005.10.011
复制
发表时间：
2006-05-01
影响因子：
4.9
通讯作者：
Peppas, NA
中科院分区：
文献类型：
--
作者：
Serra, L;Doménech, J;Peppas, NA
我们开发了一种新型的丙烯酸基聚合物，可以用于粘接输送系统。通过接枝聚乙二醇（PEG）等粘合促进剂链到聚丙烯酸水凝胶的骨架链上，对聚丙烯酸水凝胶进行了改性，从而通过互渗促进了粘合过程。合成的共聚物被命名为P（AA-g-EG）。以不同分子量的PEG（1000和2000）和不同的AA-EG的摩尔进料比（20:80,40:60,60:40,80:20,12:88,25:75,44:56,67:33）合成水凝胶。采用自由基溶液紫外光聚合法制备共聚物。采用张力试验研究了不同peg系留结构对黏附作用的影响，并计算了黏附功。由40%丙烯酸（AA）和60%乙二醇（EG）组成，含PEG 1000系链的prewollen P（AA-g-EG）共聚物薄膜的黏附作用最高，为130X10(-3) +/- 27X 10(-3) mJ，比纯PAA组成的配方高5倍。基于这些结果和相关的分子分析，我们得出结论，这种特定共聚物的高粘接性能是两种单体协同作用的结果。AA官能团允许聚合物与黏液中的糖蛋白形成多个氢键。聚乙二醇系链可能起到粘接促进剂的作用，增强聚合物链对黏液的相互渗透。(c) 2005 Elsevier B.V.版权所有
We developed novel acrylic-based polymers that can be used its mucoadhesive delivery systems. Poly(acrylic acid) hydrogels were modified by grafting adhesion promoter chains such as poly(ethylene glycol) (PEG) onto their back-bone chains, thus promoting the adhesive process by interpenetration. The copolymers synthesized were designated as P(AA-g-EG). Hydrogels were synthesized using PEG of two different molecular weights, 1000 and 2000, and with varying molar feed ratio of AA-EG (20:80, 40:60, 60:40, 80:20, 12:88, 25:75, 44:56, 67:33). The copolymers were synthesized by using free radical solution UV-polymerization. The effects of different PEG-tethered structures on mucoadhesion were studied using a tensiometric testing and the work of adhesion was calculated. Preswollen P(AA-g-EG) copolymer films composed of 40% acrylic acid (AA) and 60% ethylene glycol (EG), containing PEG 1000 tethers, exhibited the highest value for the work of mucoadhesion, 130X10(-3) +/- 27X 10(-3) mJ, that is five times higher than the formulation composed of pure PAA. Based on these results and associated molecular analysis, we conclude that the higher mucoadhesive properties of this specific copolymer were the result of the synergistic effects of both monomers. AA functional groups allowed the polymer to form multiple hydrogen bonds with the glycoproteins present in the mucus. PEG tethers possibly acted as mucoadhesive promoters, enhancing interpenetration of polymer chains into the mucus. (c) 2005 Elsevier B.V. All rights reserved.