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β-环糊精介导的从 pH 响应性果胶和普鲁兰基于水凝胶中控制释放吩噻嗪通过实验设计优化。

β-Cyclodextrin mediated controlled release of phenothiazine from pH-responsive pectin and pullulan-based hydrogel optimized through experimental design.

机构信息

Polymer and Nanomaterial Lab, Department of Chemistry, Dr B R Ambedkar National Institute of Technology, Jalandhar 144008, Punjab, India.

出版信息

Int J Biol Macromol. 2024 Oct;278(Pt 4):135045. doi: 10.1016/j.ijbiomac.2024.135045. Epub 2024 Aug 23.

DOI:10.1016/j.ijbiomac.2024.135045
PMID:39182886
Abstract

Drugs with lower permeability and water solubility provide major challenges for producing safe and efficient formulations. The current work aims to prepare ICs of the drug phenothiazine and β-cyclodextrin via physical, microwave, freeze-drying, and kneading methods. Many analytical methods, such as H NMR, ROESY, FT-IR, DSC, SEM, and XRD, were then used to confirm the formation of inclusion complexes. The natural polysaccharide-based hydrogel comprising pectin and pullulan was synthesized in air and optimized through various parameters. In order to maximize the reaction parameters, Response Surface Methodology design was employed for experimental optimization. We use FT-IR, TGA, SEM, EDX, and XRD to investigate hydrogel formation. At 37 °C, an investigation was carried out on the in vitro controlled release of PN at pH 2, 7, and 7.4. The analysis of drug release data revealed that PM and KM exhibited an initial burst release of drugs, with the MW and FD method proving to be the most suitable approach for achieving precise ICs of PN and β-CD for sustained drug release. The kinetics of drug release were evaluated using various kinetic models, with the Riteger-Peppas and Peppas-Sahlin models demonstrating the best fit for drug release in all instances.

摘要

对于具有低渗透性和低水溶性的药物来说,制备安全有效的制剂极具挑战性。本研究旨在通过物理法、微波法、冷冻干燥法和捏合法制备吩噻嗪和β-环糊精的包合物。采用 1H NMR、ROESY、FT-IR、DSC、SEM 和 XRD 等多种分析方法证实了包合物的形成。在空气中合成了基于天然多糖果胶和普鲁兰的水凝胶,并通过各种参数对其进行了优化。为了最大化反应参数,采用响应面法进行实验优化。我们使用 FT-IR、TGA、SEM、EDX 和 XRD 来研究水凝胶的形成。在 37°C 下,研究了 PN 在 pH 2、7 和 7.4 下的体外控制释放。药物释放数据分析表明,PM 和 KM 表现出药物的初始突释,MW 和 FD 法被证明是实现 PN 和β-CD 精确包合物以及持续药物释放的最适宜方法。采用各种动力学模型对药物释放动力学进行了评价,Riteger-Peppas 和 Peppas-Sahlin 模型在所有情况下均能很好地拟合药物释放。

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