de Campos Bianca Andrade, da Silva Natalia Cristina Borges, Moda Lucas Szmgel, Vidinha Pedro, Maia-Obi Lígia Passos
Center of Engineering, Modelling and Applied Social Sciences, Federal University of ABC, Avenida dos Estados, 5001, Santo André 09210-580, SP, Brazil.
Department of Fundamental Chemistry, Institute of Chemistry, University of São Paulo, Avenida Professor Lineu Prestes, 748, São Paulo 05508-000, SP, Brazil.
Polymers (Basel). 2023 Apr 5;15(7):1795. doi: 10.3390/polym15071795.
pH-sensitive degradable hydrogels are smart materials that can cleave covalent bonds upon pH variation, leading to their degradation. Their development led to many applications for drug delivery, where drugs can be released in a pH-dependent manner. Crosslinking hyperbranched polyglycerol (HPG), a biocompatible building block bearing high end-group functionality, using oxalic acid (OA), a diacid that can be synthesized from CO and form highly activated ester bonds, can generate this type of smart hydrogel. Aiming to understand the process of developing this novel material and its drug release for oral administration, its formation was studied by varying reactant stoichiometry, concentration and cure procedure and temperature; it was characterized regarding gel percent (%gel), swelling degree (%S), FTIR and thermal behavior; impregnated using ibuprofen, as a model drug, and a release study was carried out at pH 2 and 7. Hydrogel formation was evidenced by its insolubility, FTIR spectra and an increase in T and T; a pre-cure step was shown to be crucial for its formation and an increase in the concentration of the reactants led to higher %gel and lower %S. The impregnation resulted in a matrix-encapsulated system; and the ibuprofen release was negligible at pH 2 but completed at pH 7 due to the hydrolysis of the matrix. A pH-sensitive degradable HPG-OA hydrogel was obtained and it can largely be beneficial in controlled drug release applications.
pH 敏感可降解水凝胶是一种智能材料,可在 pH 值变化时切断共价键,从而导致其降解。它们的发展催生了许多药物递送应用,药物可以以 pH 依赖的方式释放。使用草酸(OA)交联超支化聚甘油(HPG),草酸是一种可由一氧化碳合成并形成高度活化酯键的二酸,HPG 是一种具有高端基官能度的生物相容性构建块,这样可以生成这种类型的智能水凝胶。为了了解这种新型材料的开发过程及其口服给药的药物释放情况,通过改变反应物的化学计量比、浓度、固化程序和温度来研究其形成过程;对其凝胶百分比(%凝胶)、溶胀度(%S)、傅里叶变换红外光谱(FTIR)和热行为进行了表征;使用布洛芬作为模型药物进行浸渍,并在 pH 为 2 和 7 的条件下进行释放研究。水凝胶的形成通过其不溶性、FTIR 光谱以及熔点(T)和玻璃化转变温度(T)的升高得以证明;预固化步骤对其形成至关重要,反应物浓度的增加会导致更高的%凝胶和更低的%S。浸渍产生了一种基质包封系统;布洛芬在 pH 为 2 时释放可忽略不计,但在 pH 为 7 时由于基质的水解而完全释放。获得了一种 pH 敏感可降解的 HPG - OA 水凝胶,它在控释药物应用中可能会有很大益处。