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在模拟肠液中从 CMC/PVA 水凝胶中靶向释放大豆肽及其药代动力学。

Targeted release of soybean peptide from CMC/PVA hydrogels in simulated intestinal fluid and their pharmacokinetics.

机构信息

State Key Laboratory of Pulp and Paper Engineering, South China University of Technology, Guangzhou 510640, China.

School of Food Science and Engineering, South China University of Technology, Guangzhou 510640, China.

出版信息

Carbohydr Polym. 2023 Jun 15;310:120713. doi: 10.1016/j.carbpol.2023.120713. Epub 2023 Feb 19.

DOI:10.1016/j.carbpol.2023.120713
PMID:36925260
Abstract

Carboxymethyl cellulose (CMC)/polyvinyl alcohol (PVA) hydrogels loaded with soybean peptide (SPE) were fabricated via a freeze-thaw method. These hydrogels conquer barriers in simulated gastric fluid (SGF), and then release SPE in simulated intestinal fluid (SIF). The results of in vitro SPE release from these hydrogels showed that in SGF only a little of the SPE released, but in SIF the SPE was completely released. The released SPE had scavenging rates for DPPH and ABTS free radicals of 41.68 and 31.43 %. The pharmacokinetic model of SPE release from the hydrogels in SIF was studied. When the hydrogels are moved from SGF to SIF, the sorption of the shrinkage hydrogel network is entirely controlled by stress-induced relaxations. There are swollen and shrunken regions during SPE release. For SPE release into the SIF, SPE has to be freed from the weak bonds in the swollen regions by changes in the conformation of CMC and PVA. The release rate of SPE was found to be governed by the diffusion and swelling rate of the shrinkage hydrogel network. The Korsmeyer-Peppas equation diffusion exponents (n) for SPE release from the hydrogels are >2.063, indicating a super case II transport. These data demonstrate CMC/PVA hydrogels have potential applications in oral peptide delivery.

摘要

羧甲基纤维素(CMC)/聚乙烯醇(PVA)水凝胶通过冻融法负载大豆肽(SPE)。这些水凝胶克服了模拟胃液(SGF)中的障碍,然后在模拟肠液(SIF)中释放 SPE。这些水凝胶中 SPE 的体外释放结果表明,在 SGF 中只有少量的 SPE 释放,但在 SIF 中 SPE 完全释放。释放的 SPE 对 DPPH 和 ABTS 自由基的清除率分别为 41.68%和 31.43%。研究了 SPE 从水凝胶在 SIF 中的释放的药代动力学模型。当水凝胶从 SGF 转移到 SIF 时,收缩水凝胶网络的吸附完全由应力诱导松弛控制。在 SPE 释放过程中有膨胀和收缩区域。对于 SPE 释放到 SIF 中,必须通过 CMC 和 PVA 的构象变化来使 SPE 从膨胀区域中的弱键中释放出来。发现 SPE 的释放速率由收缩水凝胶网络的扩散和溶胀速率控制。从水凝胶中释放 SPE 的 Korsmeyer-Peppas 方程扩散指数(n)大于 2.063,表明超二级传输。这些数据表明 CMC/PVA 水凝胶在口服肽递送上具有潜在的应用。

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