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用于控释药物递送的六肽水凝胶剂的合理设计。

Rational design of a hexapeptide hydrogelator for controlled-release drug delivery.

作者信息

Bibian Mathieu, Mangelschots Jeroen, Gardiner James, Waddington Lynne, Diaz Acevedo Maria M, De Geest Bruno G, Van Mele Bruno, Madder Annemieke, Hoogenboom Richard, Ballet Steven

机构信息

Research Group of Organic Chemistry, Vrije Universiteit Brussel, Pleinlaan 2, Brussels, B-1050, Belgium.

出版信息

J Mater Chem B. 2015 Feb 7;3(5):759-765. doi: 10.1039/c4tb01294a. Epub 2014 Dec 2.

Abstract

The amphiphilic peptide sequence H-Phe-Glu-Phe-Gln-Phe-Lys-OH (MBG-1) is developed as a novel hydrogelator for use in controlled-drug release administration, which is the smallest tunable ionic self-complementary hydrogelating peptide reported to date making it attractive for larger scale preparation. Hydrogelation is demonstrated to result from self-assembly of the peptide into beta-sheet nanofibers that are physically cross-linked by intertwining as well as larger bundle formation. Finally, the release of two small molecule cargos, fluorescein sodium and ciprofloxacin hydrochloride, is demonstrated revealing a two-stage zero-order sustained release profile up to 80% cumulative release over eight days.

摘要

两亲性肽序列H-Phe-Glu-Phe-Gln-Phe-Lys-OH(MBG-1)被开发为一种用于控释给药的新型水凝胶剂,它是迄今为止报道的最小的可调节离子自互补水凝胶化肽,这使其在大规模制备方面具有吸引力。水凝胶化被证明是由肽自组装成β-折叠纳米纤维导致的,这些纳米纤维通过缠绕以及形成更大的束而物理交联。最后,展示了两种小分子货物(荧光素钠和盐酸环丙沙星)的释放情况,揭示了一种两阶段零级持续释放曲线,在八天内累积释放高达80%。

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