Chitosan cross-linked with poly(ethylene glycol)dialdehyde via reductive amination as effective controlled release carriers for oral protein drug delivery

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• 作者：Zi-Wei Jing^a ; Zhi-Wei Ma^b ; Chen Li^a ; Yi-Yang Jia^a ; Min Luo^a ; Xi-Xi Ma^a ; Si-Yuan Zhou^a ; Bang-Le Zhang^a ; ^{blezhang@fmmu.edu.cn}
• 关键词：Chitosan ; Poly(ethylene glycol) ; Crosslinking ; Hydrogel ; Controlled delivery system
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2017
• 出版时间：15 February 2017
• 年：2017
• 卷：27
• 期：4
• 页码：1003-1006
• 全文大小：630 K
• 卷排序：27

文摘

The covalently cross-linked chitosan-poly(ethylene glycol)1540 derivatives have been developed as a controlled release system with potential for the delivery of protein drug. The swelling characteristics of the hydrogels based on these derivatives as the function of different PEG content and the release profiles of a model protein (bovine serum albumin, BSA) from the hydrogels were evaluated in simulated gastric fluid with or without enzyme in order to simulate the gastrointestinal tract conditions. The derivatives cross-linked with difunctional PEG1540-dialdehyde via reductive amination can swell in alkaline pH and remain insoluble in acidic medium. The cumulative release amount of BSA was relatively low in the initial 2 h and increased significantly at pH 7.4 with intestinal lysozyme for additional 12 h. The results proved that the release-and-hold behavior of the cross-linked CS–PEG1540H-CS hydrogel provided a swell and intestinal enzyme controlled release carrier system, which is suitable for oral protein drug delivery.