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姜黄素负载醇质体凝胶用于改善局部递药:制剂、表征及研究。

Curcumin Loaded Ethosomal Gel for Improved Topical Delivery: Formulation, Characterization and Studies.

机构信息

Department of Pharmaceutics, Delhi Pharmaceutical Sciences and Research University, New Delhi, India.

出版信息

Pharm Nanotechnol. 2021;9(4):281-287. doi: 10.2174/2211738509666210208225826.

Abstract

BACKGROUND

Curcumin is a curcuminoid, which is an active constituent of turmeric and is obtained from the rhizomes of Curcuma longa, family Zingiberaceae. Curcumin modulates the activity of various transcription factors and regulates the expression of inflammatory enzymes, cell survival proteins, adhesion molecules and cytokines by binding to a variety of proteins and inhibiting the activity of various kinases. Curcumin falls in the BCS class IV drug, with poor solubility and poor permeability which makes it very challenging to utilize the maximum therapeutic potential of this moiety Objective: The major aim of the study was to enhance transdermal penetration of curcumin via ethosomal gel and to overcome the barriers of poor permeability of transdermal drug delivery.

METHODS

Curcumin loaded ethosomes were prepared with varying quantities of ethanol and soya lecithin by the cold method and were optimised based on entrapment efficiency, vesicular size and Ex-vivo studies. Optimised ethosomal formulation was further incorporated into a gel and was evaluated. Ex-vivo studies were performed with the ethosomal gel of curcumin and was compared with simple drug solution.

RESULTS

Prepared ethosomal system showed a vesicle size ranging from 211 to 320 nm with spherical, smooth surface and entrapment efficiency of 87 to 91%. Optimised ethosomal system (ET3) was incorporated into gel and was further evaluated.

CONCLUSION

The findings of the research work suggested that the ethosomal gel holds excellent potential for transdermal delivery of curcumin.

摘要

背景

姜黄素是姜黄中的一种姜黄素,从姜黄的根茎中提取,属于姜科。姜黄素通过与多种蛋白质结合并抑制多种激酶的活性,调节各种转录因子的活性,调节炎症酶、细胞存活蛋白、粘附分子和细胞因子的表达。姜黄素属于 BCS 分类法中的第 IV 类药物,溶解度和渗透性差,这使得充分发挥该部分的治疗潜力极具挑战性。

目的

本研究的主要目的是通过醇质体凝胶提高姜黄素的经皮渗透,克服经皮给药渗透性差的障碍。

方法

采用冷法制备不同乙醇量和大豆卵磷脂量的姜黄素醇质体,并根据包封率、囊泡大小和体外研究进行优化。优化的醇质体配方进一步被纳入凝胶并进行评估。用姜黄素醇质体凝胶进行体外研究,并与简单药物溶液进行比较。

结果

所制备的醇质体系统的粒径范围为 211 至 320nm,呈球形,表面光滑,包封率为 87%至 91%。优化的醇质体系统(ET3)被纳入凝胶并进一步评估。

结论

研究工作的结果表明,醇质体凝胶具有经皮传递姜黄素的巨大潜力。

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