基于羟丙基-β-环糊精/Eudragit®EPO的双相增溶体系的开发,以增强姜黄素的溶解

IF 6.5 Q1 CHEMISTRY, APPLIED
Minghui Hao , Chungang Zhang , Ti Wang , Fantong Yu
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引用次数: 0

摘要

目的将固体分散技术与环糊精包合技术相结合,建立姜黄素双相增溶体系,以提高姜黄素的溶出度。方法以溶出度为标准,采用溶剂法制备了含有乌龙茶®EPO (EPO)和羟丙基-β-环糊精(HP-β-CD)的姜黄素复合物。通过分子对接分析了该成分的机制,随后使用傅里叶变换红外光谱(FTIR)进行了证实。此外,利用扫描电镜(SEM)、偏振光显微镜(PLM)、差示扫描量热法(DSC)和x射线衍射(XRD)等表征技术对姜黄素的组成进行了表征。结果姜黄素:EPO:HP-β-CD的溶出度为1:5:2,溶出率为100%。分子对接提示EPO的掺入增强了姜黄素与HP-β-CD的相互作用,从而稳定了体系,促进了溶解。表征结果证实该组合物以非晶形式存在。结论EPO与HP-β-CD协同使用可显著提高姜黄素的溶出率,促进其临床应用。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Development of a dual-phase solubilization system based on Hydroxypropyl-β-cyclodextrin /Eudragit® EPO for enhancing the dissolution of curcumin

Development of a dual-phase solubilization system based on Hydroxypropyl-β-cyclodextrin /Eudragit® EPO for enhancing the dissolution of curcumin

Objective

This research aims to establish a dual-phase solubilization system for curcumin by combining solid dispersion technology with cyclodextrin inclusion technology, in order to improve the dissolution of curcumin.

Methods

A composition of curcumin containing Eudragit® EPO (EPO) and Hydroxypropyl-β-cyclodextrin (HP-β-CD) was prepared using the solvent method, with the dissolution rate serving as the criterion for identifying the optimal formulation. The mechanism underlying this composition was analyzed through molecular docking, which were later corroborated using Fourier transform infrared spectroscopy (FTIR). Furthermore, various characterization techniques including scanning electron microscopy (SEM), polarized light microscopy (PLM), differential scanning calorimetry (DSC), and X-ray diffraction (XRD) were employed to examine the characteristics of the curcumin composition.

Results

The investigations on dissolution revealed that the optimal formulation consists of curcumin:EPO:HP-β-CD in a ratio of 1:5:2, achieving an impressive 100 %. Molecular docking suggested that the incorporation of EPO enhances the interaction between curcumin and HP-β-CD, thereby stabilizing the system and facilitating improved dissolution. Characterization results affirmed that the composition is present in an amorphous form.

Conclusion

The synergistic use of EPO and HP-β-CD significantly enhanced the dissolution rate of curcumin, thereby potentially facilitating its clinical application.
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