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作为用于旨在治疗孢子丝菌病的绿色提取物递送系统的局部纳米乳剂

Topical Nanoemulsions as Delivery Systems for Green Extracts of Aiming at the Treatment of Sporotrichosis.

作者信息

Medeiros-Neves Bruna, Heidrich Daiane, Schuh Roselena Silvestri, Brazil Nathalya Tesch, Fachel Flávia Nathiely Silveira, Cassel Eduardo, Vargas Rubem Mário Figueiró, Scroferneker Maria Lúcia, von Poser Gilsane Lino, Koester Letícia Scherer, Teixeira Helder Ferreira

机构信息

Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Av. Ipiranga 2752, Porto Alegre 90610-000, RS, Brazil.

Departamento de Microbiologia, ICBS, Universidade Federal do Rio Grande do Sul, Rua Sarmento Leite, Porto Alegre 90050-170, RS, Brazil.

出版信息

Pharmaceutics. 2024 Apr 2;16(4):492. doi: 10.3390/pharmaceutics16040492.

Abstract

Coumarins are benzopyrones found in several plant genera, including (Asteraceae). These compounds represent an important source of new treatments, especially as antimicrobial and antifungal agents. In this study, two coumarin-rich extracts from using green technologies were obtained through aqueous maceration (AE) and supercritical fluid extraction (SFE). Such extracts were incorporated into nanoemulsions (NAE and NSFE) composed of a medium-chain triglyceride oil core stabilized by phospholipids. The nanoemulsions exhibited droplet sizes between 127 and 162 nm, pH above 5.0, and viscosity of approximately 1.0 cP, properties compatible with the topical route. The coumarins permeation/retention from formulations through ear porcine skin using Franz-type diffusion cells were evaluated. Whatever the extract, coumarins were distributed in skin layers, especially in the dermis in both intact and impaired (tape stripping) skin. In addition, a significant increase in coumarins that reached up to the receptor fluid was observed for impaired skin, with increases of approximately threefold for NAE and fourfold for NSFE. Finally, antifungal activity of nanoemulsions was evaluated according to minimum inhibitory concentrations, and the values were 250 µg/mL for all strains tested. The overall results demonstrated the feasibility of incorporating extracts into nanoemulsions and showed a potential alternative for the treatment of sporotrichosis.

摘要

香豆素是存在于包括土木香属(菊科)在内的多个植物属中的苯并吡喃类化合物。这些化合物是新治疗方法的重要来源,尤其是作为抗菌和抗真菌剂。在本研究中,通过水浸提法(AE)和超临界流体萃取法(SFE),利用绿色技术从土木香中获得了两种富含香豆素的提取物。这些提取物被掺入由磷脂稳定的中链甘油三酯油核组成的纳米乳剂(NAE和NSFE)中。纳米乳剂的液滴尺寸在127至162nm之间,pH值高于5.0,粘度约为1.0cP,这些性质与局部给药途径相兼容。使用Franz型扩散池评估了制剂中香豆素通过猪耳皮肤的渗透/滞留情况。无论使用哪种提取物,香豆素都分布在皮肤层中,尤其是在完整皮肤和受损(胶带剥离)皮肤的真皮层中。此外,观察到受损皮肤中到达受体液的香豆素显著增加,NAE增加了约三倍,NSFE增加了四倍。最后,根据最低抑菌浓度评估了纳米乳剂的抗真菌活性,所有测试菌株的值均为250μg/mL。总体结果证明了将土木香提取物掺入纳米乳剂的可行性,并显示出治疗孢子丝菌病的潜在替代方法。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/85d2/11054391/a7bdca0d7bcf/pharmaceutics-16-00492-g001.jpg

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