姜黄素负载水溶性固体分散体局部凝胶的开发和评价:一种更绿色的药物透皮给药方法

IF 1.1 Q3 CHEMISTRY, MULTIDISCIPLINARY
Devika Tripathi, Sangeeta Mishra, A. Rai, Jagannath Sahoo, D. Sharma, Yadvendra Singh
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引用次数: 1

摘要

姜黄素的水溶性差仍然是一个挑战。由于姜黄素在溶解溶剂中的不稳定性,在溶液中使用不可持续的溶剂和溶解氧可能是个问题。因此,考虑到所有事实,需要寻找一种有前途的替代溶剂介质。事实上,最近已经评估了一种亲水剂的溶液。亲水剂是有机溶剂的最佳替代品。这些是环保、安全、无毒的制剂。因此,本研究的重点是通过亲水性固体分散方法提高姜黄素的溶解度。令人惊讶的是,姜黄素在水杨酸钠水溶性溶液中显示出显著的溶解度增强。水杨酸钠水凝胶确保了姜黄素在溶液中的稳定性,保持了均匀性,并表现出抗氧化性能。水溶液法和固体分散技术相结合是提高姜黄素生物利用度的一种简单有效的方法。开发了负载姜黄素的水热性固体分散体局部凝胶,以实现姜黄素的透皮递送。通过溶剂蒸发法制备固体分散体,并评价其体外性能。对制备的HSD进行了体外溶出度、药物含量、FTIR和XRD分析。通过分散法将选定的HSD(1:4)加载到局部凝胶中,并进行体外参数,如药物含量、可传播性、pH、药物溶解速率和药物含量。溶解度研究大大提高了姜黄素在2M水杨酸钠水溶性溶液中的溶解度。水杨酸钠与固体分散体的配方相容。成功地以1:4的比例制备了水热性固体分散体。XRD结果表明姜黄素在苯甲酸钠存在下具有无定形性质。溶出度研究表明,与纯姜黄素和PM(1:4)相比,释放度有所提高。然后通过使用卡波姆934和羟丙基甲基纤维素作为胶凝剂的分散法将制备的HSD掺入凝胶中。Cur-HSD凝胶外观均匀透明。该凝胶在120分钟内显示出优异的铺展性和94.2的药物含量,药物释放率为90.21%,并且在存在水溶性聚合物的情况下显示出改善的释放,以改善姜黄素的局部递送。因此,为了增强难溶性植物成分的局部递送,水凝胶被认为是一种更环保的方法,并可用于其他难溶性的植物成分。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Curcumin-loaded hydrotropic solid dispersion topical gel development and evaluation: A greener approach towards transdermal delivery of drugs
Curcumin's poor water solubility still presents a challenge. Because of Curcumin's instability in solubilizing solvents, using a non-sustainable solvent and dissolved oxygen in the Solution might be the problem. Thus, considering all facts, looking for a promising alternative solvent medium is in need. Indeed, a solution of hydrotropic agent has been assessed recently. Hydrotropic agents are the best replacements for organic solvents. These are eco-friendly, safe, and non-toxic agents. Hence, the presented research focuses on improving the solubility of Curcumin through a hydrotropic solid dispersion approach. Amazingly, Curcumin showed a significant solubility enhancement in sodium salicylate hydrotropic Solution. Sodium salicylate hydrotrope ensured the stability of Curcumin in Solution, maintained homogeneity, and exhibited antioxidant properties. Hydrotropy combined with the solid dispersion technique is a simple and effective way to improve the bioavailability of Curcumin. Hydrotropic solid dispersion loaded curcumin topical gel was developed to achieve transdermal delivery of Curcumin. Solid dispersion was prepared by solvent evaporation method and evaluated for in-vitro performance. In-vitro drug dissolution, drug content, FTIR, and XRD were carried out for the prepared HSD. The selected HSD (1:4) was loaded into a topical gel by dispersion method, and in-vitro parameters like drug content, Spreadability, pH, rate of drug dissolution, and drug content were performed. The solubility study has substantially enhanced the solubility of Curcumin in a 2M sodium salicylate hydrotropic solution. Sodium salicylate was compatible with formulating the solid dispersion. Hydrotropic solid dispersion was successfully prepared in 1:4 ratios. XRD results have shown the amorphous nature of Curcumin in the presence of sodium benzoate. The dissolution studies have shown improved release compared to pure Curcumin and PM (1:4). The prepared HSD was then incorporated into a gel by dispersion method using carbopol 934 and hydroxypropyl methylcellulose as a gelling agent. The Cur-HSD gel was homogeneous and transparent in appearance. The gel showed excellent Spreadability and drug content of 94.2 with 90.21% of percent drug release for 120 min and showed improved release in the presence of hydrotrope for improved topical delivery of Curcumin. Thus, to enhance the topical delivery of poorly soluble phytoconstituents, hydrotropes are suggested as a greener approach and to be applied for other poorly soluble phytoconstituents.
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来源期刊
Current Green Chemistry
Current Green Chemistry CHEMISTRY, MULTIDISCIPLINARY-
CiteScore
4.30
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13.60%
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6
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