应用液固技术提高姜黄素溶解度:一项中心复合设计研究

IF 2.2 4区 化学 Q2 Engineering
Sareh Aghajanpour, Shabnam Yousefi Jordehi, Ali Farmoudeh, Reza Negarandeh, Matthew Lam, Pedram Ebrahimnejad, Ali Nokhodchi
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引用次数: 0

摘要

姜黄,特别是姜黄素(C21H20O6)等姜黄类化合物,具有广泛的治疗功效,包括抗炎、抗癌和抗衰老特性。然而,姜黄素的疏水性导致其生物利用率较低,从而大大限制了其临床疗效。本研究旨在通过开发液固型紧密分散制剂来提高姜黄素的溶解度和生物利用度。针对姜黄素有限的水溶性(25 °C时为3.12 mg/l)和高油水分配系数(\(\text{log}Kow=3.29\)),我们采用了中心复合设计(CCD)来优化液态固体紧密分散制剂。优化的重点是片剂的物理性质,如硬度、崩解时间和 30 分钟的溶出率。关键配方成分包括作为液体载体的吐温 80 和作为包衣材料的 Aerosil 200,它们是优化过程中的自变量。优化后的配方含有 30 毫克 Tween 80 和 75 毫克 Aerosil 200,显著提高了姜黄素的溶出率。实验结果证实了该配方的有效性,与传统配方的 300 分钟相比,该配方将 63.2% 的药物溶解时间明显缩短至 165 分钟。差示扫描量热法和傅立叶变换红外光谱显示,姜黄素转变为非结晶状态,并与吐温 80 形成氢键,从而提高了溶解度。这项研究成功地展示了通过液态固体紧密分散制剂提高姜黄素生物利用度的可行策略。通过解决姜黄素的溶解性难题,该技术在提高 BCS II 类和 IV 类药物的临床适用性方面取得了重大进展,可能会为广泛的治疗应用带来益处。 图解摘要利用中心复合设计(CCD)方法优化姜黄素液态固体制剂的图解表示
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Applying liquisolid technique to enhance curcumin solubility: a central composite design study

Turmeric, specifically its curcuminoids such as curcumin (C21H20O6), possesses extensive therapeutic benefits including anti-inflammatory, anticancer, and anti-aging properties. However, curcumin’s clinical effectiveness is significantly limited by its hydrophobic nature, leading to poor bioavailability. This study aims to enhance the solubility and bioavailability of curcumin through the development of liquisolid compact dispersion formulations. To address curcumin’s limited water solubility (3.12 mg/l at 25 °C) and high oil–water partition coefficient (\(\text{log}Kow=3.29\)), we employed a central composite design (CCD) to optimize liquisolid compact dispersion formulations. The optimization focused on the tablet’s physical properties, such as hardness, disintegration time, and dissolution rate at 30 min. Critical formulation components included Tween 80 as the liquid vehicle and Aerosil 200 as the coating material, serving as independent variables in the optimization process. The optimized formulation, containing 30 mg of Tween 80 and 75 mg of Aerosil 200, significantly improved curcumin’s dissolution rate. Experimental results confirmed the formulation’s effectiveness, with a marked reduction in the time to dissolve 63.2% of the drug to 165 min, compared to 300 min for conventional formulations. Differential scanning calorimetry and Fourier-transform infrared spectra indicated a transformation of curcumin into a non-crystalline state and the formation of hydrogen bonds with Tween 80, contributing to enhanced solubility. This study successfully demonstrates a viable strategy to enhance the bioavailability of curcumin through liquisolid compact dispersion formulations. By addressing the solubility challenges of curcumin, this technique presents a significant advancement in improving the clinical applicability of BCS class II and IV drugs, potentially benefiting a wide range of therapeutic applications.

Graphical abstract

Graphical representation of optimizing curcumin liquisolid formulation using central composite design (CCD) methodology

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来源期刊
Chemical Papers
Chemical Papers Chemical Engineering-General Chemical Engineering
CiteScore
3.30
自引率
4.50%
发文量
590
期刊介绍: Chemical Papers is a peer-reviewed, international journal devoted to basic and applied chemical research. It has a broad scope covering the chemical sciences, but favors interdisciplinary research and studies that bring chemistry together with other disciplines.
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