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首页> 外文期刊>International Journal of Pharmaceutics >Modeling of small-molecule release from crosslinked hydrogel microspheres: effect of crosslinking and enzymatic degradation of hydrogel matrix.
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Modeling of small-molecule release from crosslinked hydrogel microspheres: effect of crosslinking and enzymatic degradation of hydrogel matrix.

机译：从交联的水凝胶微球中释放小分子的模型：水凝胶基质的交联和酶促降解作用。

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摘要

A diffusion-based model describing the drug release from a charged hydrogel (gelatin) microsphere undergoing enzymatic degradation is presented. The model elucidates the effect of glutaraldehyde, a crosslinking agent, on the release profile in terms of the initial drug distribution, diffusivity of the drug, degradation rate of gelatin and its ability to form polyionic complex with the drug. The model was validated by comparing with in vitro release of trypan blue, an acidic model drug, from basic gelatin microspheres. While drug release was not a simple function of glutaraldehyde concentration, the effective diffusivity was found to be inversely proportional to glutaraldehyde concentration in the form of a power function when the initial drug distribution was taken into consideration. For these reasons, the present model can accurately predict drug release with no adjustable parameters, given the collagenase concentration. The present model may help design certain release scenarios from biodegradable charged hydrogels for the oppositely charged drugs and biomolecules.
机译：提出了一种基于扩散的模型，该模型描述了从经过酶促降解的带电水凝胶（明胶）微球中释放的药物。该模型从初始药物分布，药物的扩散性，明胶的降解速率及其与药物形成聚离子复合物的能力等方面阐明了戊二醛（一种交联剂）对释放曲线的影响。通过与从碱性明胶微球体外释放酸性模型药物锥虫蓝的比较来验证该模型。虽然药物释放不是戊二醛浓度的简单函数，但是当考虑初始药物分布时，发现有效扩散率与幂函数​​形式的戊二醛浓度成反比。由于这些原因，在给定胶原酶浓度的情况下，本模型可以在没有可调参数的情况下准确预测药物释放。本模型可以帮助设计带相反电荷的药物和生物分子的可生物降解的带电荷水凝胶的某些释放方案。

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