微针辅助有机凝胶配方提高姜黄素的透皮给药效果

Sushruta Mulay, D. Mehta
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摘要

姜黄素是姜黄中的一种天然化合物,已被证明具有抗炎和抗氧化特性。通过有机乳液凝胶外用姜黄素可以有效针对人体特定部位的炎症。本研究旨在配制基于 Pluronic 的姜黄素有机凝胶,并通过微针技术进一步帮助其吸收。研究人员制备了九种有机凝胶配方,并通过 32 全因子模型进行了优化,以确定卵磷脂[A]和 Pluronic[B]的浓度比例,从而获得 2 小时后的最佳药物释放量(Q2)和 8 小时后的最大药物释放量(Q8)。通过弗兰兹扩散池进行的体外研究表明,Pluronic F-127 浓度对药物释放有显著影响。随着 Pluronic 浓度的增加,制剂的粘度也随之增加,最终导致药物释放缓慢。根据实验设计(DoE)研究,进一步研究了含有 6.5% 卵磷脂和 20.6% Pluronic 的优化批次在微针辅助下通过大鼠皮肤的体外渗透情况。8 小时后,无微针孔化的渗透率约为 70.26%,经微针处理后,渗透率显著增加(约 25%)。结果表明,微针辅助皮肤渗透作为一种非侵入性和可控的姜黄素透皮给药途径的应用前景广阔。建议进一步开展体内研究,以进一步确立这一前景广阔的概念,通过非侵入性透皮给药系统治疗各种炎症,包括关节炎、牛皮癣和湿疹等。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Microneedles Assisted Enhancement of Transdermal Delivery of Curcumin through Organogel Formulation
Curcumin is a natural compound found in turmeric and has been shown to have anti-inflammatory and antioxidant properties. Topical delivery of curcumin through an organic emulsion-based gel can effectively target inflammation at specific sites on the body. The current study aims to formulate Pluronic based organogel of curcumin, whose absorption is further assisted by microneedles technology. Nine organogel formulations were prepared and optimized by 32 full factorization model to fix the ratio of lecithin[A] and Pluronic[B] concentration in order to get optimum drug release after 2 hours (Q2) and maximum release of drug after 8 hours (Q8). The in-vitro study through the Franz diffusion cell indicated a significant impact of Pluronic F-127 concentration on the release of drug. As increased concentration of Pluronic increased the viscosity of formulations which ultimately retarded the release of drug. Based on Design of Experiment (DoE) study, optimized batch containing 6.5% lecithin and 20.6% Pluronic was further studied for microneedle assisted ex-vivo skin permeation through rat skin. Permeation without microneedle poration was around 70.26% after 8 hours, which was significantly increased (around 25%) after microneedle treatment of the skin. The results indicated promising application microneedle assisted skin permeation as a non-invasive and controlled delivery of curcumin through the transdermal route. Further, in-vivo studies are recommended to further establish this promising concept, targeting a variety of inflammatory conditions, including arthritis, psoriasis, and eczema, etc., through non-invasive transdermal drug delivery systems.
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