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(2-羟丙基)-β-环糊精介导的罗望子籽粉/κ-卡拉胶水凝胶中依达拉奉的持续释放:微波辅助合成及实验设计优化。

Sustained release of edaravone from (2-hydroxypropyl)-β-cyclodextrin mediated tamarind kernel powder/kappa-carrageenan hydrogel: Microwave-assisted synthesis and optimization using experimental design.

机构信息

Polymer and Nanomaterial Lab, Department of Chemistry, Dr. BR Ambedkar National Institute of Technology, Jalandhar 144011, Punjab, India.

出版信息

Int J Biol Macromol. 2022 Oct 31;219:246-261. doi: 10.1016/j.ijbiomac.2022.07.237. Epub 2022 Aug 3.

DOI:10.1016/j.ijbiomac.2022.07.237
PMID:35932803
Abstract

In the current study, a sustained release formulation made of natural polysaccharide tamarind kernel powder/kappa-carrageenan and (2-hydroxypropyl)-β-cyclodextrin (2-Hp-β-CD) was chosen to increase drug effectiveness. A kappa-carrageenan and tamarind kernel powder 3-D hydrogel network was synthesized with the aid of microwave irradiations. The ICs complexes were prepared using a physical mixture (PM), kneading (KM), and microwave (MW) approach and were then successfully loaded into the hydrogel. The synthesis of ICs was verified as a true IC using DSC, SEM, FTIR, H NMR, and 2D NMR ROESY. A study on the in vitro sustained release of EV at pH 2, 7, and 7.4 was conducted at 37 °C. The microwave (MW) method was the most effective method for preparing true ICs of EV and 2-Hp-β-CD for sustained drug release, as evidenced by the drug release data, which indicated that PM and KM displayed a burst release of the drug. Ritger-Peppas and Peppas-Sahlin were essential models for drug release. A phase solubility analysis was done to evaluate the IC's stoichiometry and complexation constant. Studies on drug release have shown that 2-Hp-β-CD was effective at causing pH-responsive sustained drug release.

摘要

在本研究中,选择了由天然多糖罗望子种子粉/κ-卡拉胶和(2-羟丙基)-β-环糊精(2-Hp-β-CD)制成的缓释制剂来提高药物的有效性。在微波辐射的辅助下,合成了κ-卡拉胶和罗望子种子粉 3-D 水凝胶网络。使用物理混合物(PM)、捏合(KM)和微波(MW)方法制备了 ICs 复合物,然后成功地将其负载到水凝胶中。使用 DSC、SEM、FTIR、H NMR 和 2D NMR ROESY 验证了 ICs 的合成是真正的 IC。在 37°C 下,在 pH 2、7 和 7.4 下进行了 EV 的体外缓释研究。从药物释放数据可以看出,MW 方法是制备 EV 和 2-Hp-β-CD 真正 ICs 以实现持续药物释放的最有效方法,表明 PM 和 KM 表现出药物的突释。Ritger-Peppas 和 Peppas-Sahlin 是药物释放的重要模型。进行了相溶解度分析以评估 IC 的化学计量和络合常数。药物释放研究表明,2-Hp-β-CD 有效引发 pH 响应的持续药物释放。

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