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基于聚(甲基乙烯基醚-共-马来酸)和吐温 85 的水凝胶用于疏水性药物的持续释放。

Hydrogels based on poly(methyl vinyl ether-co-maleic acid) and Tween 85 for sustained delivery of hydrophobic drugs.

机构信息

School of Pharmacy, Queens University Belfast, Medical Biology Centre, 97 Lisburn Road, Belfast BT9 7BL, Northern Ireland, UK.

School of Pharmacy, Queens University Belfast, Medical Biology Centre, 97 Lisburn Road, Belfast BT9 7BL, Northern Ireland, UK.

出版信息

Int J Pharm. 2018 Mar 1;538(1-2):147-158. doi: 10.1016/j.ijpharm.2018.01.025. Epub 2018 Jan 17.

Abstract

Hydrogels based on poly(methyl vinyl ether-co-maleic acid) and Tween 85 were prepared for hydrophobic drug delivery. The hydrogels were synthesized following a simple procedure carried out in solid state. The process did not require the use of any solvent and, as it is based on an esterification reaction, no toxic by-products were obtained. The resulting hydrogels contained Tween 85 inside the structure and due to the amphiphilic nature of this compound, hydrophobic domains within the hydrogel structure were formed. The obtained hydrogels showed good swelling capacities ranging from 100% to 600%. The esterification reaction that took place between poly(methyl vinyl ether-co-maleic acid) and Tween 85 was confirmed by infrared spectroscopy. Hydrogels were loaded with a hydrophobic drug model, Curcumin (CUR), showing that the hydrogels were able to retain up to 36 mg of CUR per g of hydrogel. Additionally, the synthesized hydrogels provided in vitro sustained CUR release over periods of up to 30 days. Finally, and due to the mucoadhesive nature of the prepared materials, one of the hydrogels was tested in vitro as an oral drug delivery system. For this purpose, the selected material was milled into microparticles (45-90 µm diameter). The release of CUR from the microparticles was evaluated under simulated gastric and intestinal conditions. The microparticles were able to release their cargos in 7 h. However, further work is required to optimize this system for oral drug delivery applications.

摘要

基于聚(甲基乙烯基醚-共-马来酸)和吐温 85 的水凝胶被制备用于疏水性药物递送。水凝胶是通过在固态下进行的简单程序合成的。该过程不需要使用任何溶剂,并且由于它基于酯化反应,因此没有获得有毒的副产物。所得水凝胶在结构内包含吐温 85,由于该化合物的两亲性质,在水凝胶结构内形成了疏水性域。所获得的水凝胶显示出从 100%到 600%的良好溶胀能力。聚(甲基乙烯基醚-共-马来酸)和吐温 85 之间发生的酯化反应通过红外光谱得到证实。水凝胶被加载疏水性药物模型姜黄素(CUR),表明水凝胶能够保留每克水凝胶多达 36mg 的 CUR。此外,合成的水凝胶在长达 30 天的时间内提供了 CUR 的体外持续释放。最后,由于制备的材料具有粘膜粘附性,其中一种水凝胶被测试作为口服药物递送系统的体外。为此,选择的材料被研磨成微颗粒(45-90μm 直径)。在模拟的胃和肠条件下评估了 CUR 从微颗粒中的释放。微颗粒能够在 7 小时内释放其货物。然而,需要进一步的工作来优化该系统用于口服药物递送应用。

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