黄檀和姜黄协同植物成分的创新透皮给药：配方、表征和生物功效

IF 2.7 4区医学 Q2 PHARMACOLOGY & PHARMACY

Journal of Pharmaceutical Innovation Pub Date : 2025-10-01 DOI:10.1007/s12247-025-10106-4

Vishnu Das, Joohee Pradhan

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引用次数: 0

摘要

目的黄檀和姜黄具有抗炎和伤口愈合的作用；然而，它们的关键植物成分表现出较差的水溶性和有限的膜透性，限制了透皮功效。本研究旨在开发和评估这些提取物的透皮溶酶体凝胶（TEGs），以增强皮肤渗透，伤口修复和抗炎活性，采用质量设计（QbD）方法。方法采用Box-Behnken设计法，对龙骨草（PECL）和龙骨草（PEDS）粉末提取物的颗粒大小和包封效率进行优化。将优化后的配方（F6）掺入3种teg （G1-G3; pH 7.4、7.0和5.5）中，并与非乙醇体凝胶（NG）进行比较。进行了理化特性、体外释放（Franz扩散细胞）、体内伤口愈合（切除模型）和抗炎活性（卡拉胶诱导的足跖水肿）的研究。分子对接评估了植物成分与hTNF-α的相互作用。结果f6具有小泡大小（PEDS: 110±4.78 nm; PECL: 100±3.05 nm; PDI < 0.15）、高包封效率（~ 98%）和稳定的zeta电位（- 50.2 mV）。G3 (pH 5.5) 6 h释药率最高，PEDS为96.14%，PECL为98.64%。TG3在体内第8天创面愈合率为98.47±0.82%，第12天创面完全愈合，上皮形成时间最短（7天），显著优于NG （p < 0.01）。TG3也表现出最高的抗炎作用（360 min时抑制69.3%,p < 0.01 vs. NG）。对接研究证实了黄檀素和姜黄素与hTNF-α的强结合，与观察到的生物活性相关。结论：ph5.5 TEG可显著增强经皮递送、伤口愈合和抗炎作用，强调其作为炎症性皮肤疾病治疗候选药物的潜力。图形抽象

本文章由计算机程序翻译，如有差异，请以英文原文为准。

Innovative Transdermal Delivery of Synergistic Phytoconstituents from Dalbergia Sissoo and Curcuma Longa: Formulation, Characterization, and Biological Efficacy

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Innovative Transdermal Delivery of Synergistic Phytoconstituents from Dalbergia Sissoo and Curcuma Longa: Formulation, Characterization, and Biological Efficacy

Purpose

Dalbergia sissoo and Curcuma longa possess established anti-inflammatory and wound-healing properties; however, their key phytoconstituents exhibit poor aqueous solubility and limited membrane permeability, restricting transdermal efficacy. This study aimed to develop and evaluate transdermal ethosomal gels (TEGs) of these extracts to enhance skin penetration, wound repair, and anti-inflammatory activity using a Quality by Design (QbD) approach.

Methods

Ethosomal formulations of powdered extracts of D. sissoo (PEDS) and C. longa (PECL) were optimized via Box–Behnken Design for particle size and entrapment efficiency. The optimized formulation (F6) was incorporated into three TEGs (G1–G3; pH 7.4, 7.0, and 5.5) and compared with a non-ethosomal gel (NG). Physicochemical characterization, in vitro release (Franz diffusion cell), in vivo wound healing (excision model), and anti-inflammatory activity (carrageenan-induced paw edema) were performed. Molecular docking assessed phytoconstituent interactions with hTNF-α.

Results

F6 displayed small vesicle sizes (PEDS: 110 ± 4.78 nm; PECL: 100 ± 3.05 nm; PDI < 0.15), high entrapment efficiency (~ 98%), and stable zeta potential (− 50.2 mV). G3 (pH 5.5) showed the highest drug release (PEDS: 96.14%; PECL: 98.64% at 6 h). In vivo, TG3 achieved 98.47 ± 0.82% wound closure by day 8, complete closure by day 12, and the shortest epithelization period (7 days), significantly outperforming NG (p < 0.01). TG3 also exhibited the highest anti-inflammatory effect (69.3% inhibition at 360 min, p < 0.01 vs. NG). Docking studies confirmed strong hTNF-α binding by dalbergin and curcuminoids, correlating with observed biological activity.

Conclusion

G3 (pH 5.5 TEG) significantly enhances transdermal delivery, wound healing, and anti-inflammatory effects, underscoring its potential as therapeutic candidate for inflammatory skin conditions.

Graphical Abstract

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来源期刊

Journal of Pharmaceutical Innovation PHARMACOLOGY & PHARMACY-

CiteScore

3.70

自引率

3.80%

发文量

审稿时长

>12 weeks

期刊介绍： The Journal of Pharmaceutical Innovation (JPI), is an international, multidisciplinary peer-reviewed scientific journal dedicated to publishing high quality papers emphasizing innovative research and applied technologies within the pharmaceutical and biotechnology industries. JPI''s goal is to be the premier communication vehicle for the critical body of knowledge that is needed for scientific evolution and technical innovation, from R&D to market. Topics will fall under the following categories: Materials science, Product design, Process design, optimization, automation and control, Facilities; Information management, Regulatory policy and strategy, Supply chain developments , Education and professional development, Journal of Pharmaceutical Innovation publishes four issues a year.