Devices based on intelligent biopolymers for oral protein delivery
Devices based on intelligent biopolymers for oral protein delivery
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DOI：
10.1016/j.ipharm.2003.03.001
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发表时间：
2004-06-11
影响因子：
5.8
通讯作者：
Peppas, NA
中科院分区：
文献类型：
--
作者：
Peppas, NA
生物粘附控制药物递送的主要目标是将递送装置定位在体内以以位点特异性方式增强药物吸收过程。良好粘附性的重要贡献者是分子粘附促进剂的存在，例如聚合物系链结构（例如，接枝到交联网络上的聚（乙二醇）链）或甚至自由扩散穿过凝胶/凝胶界面的线性链。最近，我们已经开发了一类非常有前途的药物，特别是蛋白质递送载体。聚（甲基丙烯酸）接枝与聚（乙二醇）的共聚物网络表现出可逆的，pH值依赖性的溶胀行为，由于质子化的侧酸基团和接枝链上的醚基团之间的共聚体复合物的形成。含有等摩尔量的MAA/EG的凝胶在低pH值下表现出最低的溶胀度增加络合。溶胀溶液的pH值对平均网络网孔尺寸或相关长度有显著影响。胰岛素从含有分子量1000的PEG接枝物的P（MAA-g-EG）凝胶中的体外释放表明，随着凝胶解络合和胰岛素通过结构释放，胰岛素显著释放。另外的体外研究结果表明，胰岛素释放速率可以通过适当调整凝胶的结构来控制。(C)2004 Elsevier B. V.保留所有权利。
The primary goal of bioadhesive controlled drug delivery is to localize a delivery device within the body to enhance the drug absorption process in a site-specific manner. An important contributor to good adhesion is the presence of molecular adhesion promoters such as polymer-tethered structure (e.g., poly(ethylene glycol) chains grafted to crosslinked networks) or even linear chains which are free to diffuse across the gel/gel interface. Recently, we have developed a very promising class of carriers for drug and especially protein delivery. Copolymer networks of poly(methacrylic acid) grafted with poly(ethylene glycol) exhibit reversible, pH-dependent swelling behavior due to the formation of interpolymer complexes between protonated pendant acid groups and the etheric groups on the graft chains. Gels containing equimolar amounts of MAA/EG exhibited the lowest degree of swelling at low pH increased complexation. The average network mesh size or correlation length was dramatically affected by the pH of the swelling solution. The in vitro release of insulin from P(MAA-g-EG) gels containing PEG grafts of molecular weight 1000 indicates a significant release of insulin as the gel decomplexes and insulin is freed through the structure. The results of additional in vitro studies have shown that insulin release rates can be controlled by appropriate adjustment of the structure of the gels. (C) 2004 Elsevier B.V. All rights reserved.