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基于聚丙烯酰胺和聚(β-二甲基氨基乙基甲基丙烯酸酯)的半互穿网络冷冻凝胶的制备与表征;用单氯代三嗪基-β-环糊精对载体进行功能化及姜黄素的释放动力学。

Preparation and Characterization of Semi-IPN Cryogels Based on Polyacrylamide and Poly(,-dimethylaminoethyl methacrylate); Functionalization of Carrier with Monochlorotriazinyl-β-cyclodextrin and Release Kinetics of Curcumin.

机构信息

Department of Functional Polymers, "Petru Poni" Institute of Macromolecular Chemistry, 700487 Iași, Romania.

出版信息

Molecules. 2021 Nov 18;26(22):6975. doi: 10.3390/molecules26226975.

Abstract

Curcumin (CCM) is a natural hydrophobic polyphenol known for its numerous applications in the food industry as a colorant or jelly stabilizer, and in the pharmaceutical industry due to its anti-inflammatory, antibacterial, antioxidant, anti-cancer, and anti-Alzheimer properties. However, the large application of CCM is limited by its poor solubility in water and low stability. To enhance the bioavailability of CCM, and to protect it against the external degradation agents, a novel strategy, which consists in the preparation of semi-interpenetrating polymer networks, (s-IPNs) based on poly(,-dimethylaminoethyl methacrylate) entrapped in poly(acrylamide) networks, by a cryogelation technique, was developed in this work. All s-IPN cryogels were characterized by SEM, EDX, FTIR, and swelling at equilibrium as a function of pH. Functionalization of semi-IPN cryogel with monochlorotriazinyl-β-cyclodextrin (MCT-β-CD) led to IPN cryogel. The release profile of CCM from the composite cryogels was investigated at 37 °C, in pH 3. It was found that the cumulative release increased with the increase of the carrier hydrophobicity, as a result of increasing the cross-linking degree, the content and the molar mass of PDMAEMA. Fitting Higuchi, Korsmeyer-Peppas, and first order kinetic models on the CCM release profiles indicated the diffusion as the main driving force of drug release from the composite cryogels.

摘要

姜黄素(CCM)是一种天然疏水性多酚,因其在食品工业中的多种应用而闻名,例如作为着色剂或果冻稳定剂,以及在制药工业中因其具有抗炎、抗菌、抗氧化、抗癌和抗阿尔茨海默病的特性。然而,CCM 的广泛应用受到其在水中的溶解度差和稳定性低的限制。为了提高 CCM 的生物利用度,并保护其免受外部降解剂的影响,本工作开发了一种新策略,即通过冷冻凝胶技术制备基于聚(,-二甲基氨基乙基甲基丙烯酸酯)的半互穿聚合物网络(s-IPN),该聚合物被包埋在聚丙烯酰胺网络中。所有 s-IPN 冷冻凝胶均通过 SEM、EDX、FTIR 和在 pH 值下的平衡溶胀进行了表征。用一氯三嗪基-β-环糊精(MCT-β-CD)对半 IPN 冷冻凝胶进行功能化,得到 IPN 冷冻凝胶。在 37°C、pH 3 下研究了 CCM 从复合冷冻凝胶中的释放情况。结果发现,随着载体疏水性的增加,累积释放量增加,这是由于交联度、PDMAEMA 的含量和摩尔质量的增加所致。将 Higuchi、Korsmeyer-Peppas 和一级动力学模型拟合到 CCM 的释放曲线表明,扩散是药物从复合冷冻凝胶中释放的主要驱动力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/af88/8622513/2ca0d0b02056/molecules-26-06975-g001.jpg

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