自纳米乳化给药系统增强艾非那康唑对红毛癣菌和红毛癣菌的渗透和活性。

IF 5.5 3区 医学 Q1 PHARMACOLOGY & PHARMACY
Seo Wan Yun, Jeong Gyun Lee, Chul Ho Kim, Kyeong Soo Kim
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引用次数: 0

摘要

背景:甲真菌病对局部治疗反应不佳,而依非那康唑(EFN)的水溶性较低。方法:制备一种溶解度、渗透性、抗真菌活性和稳定性均得到改善的10% w/w EFN自纳米乳化体系(SNEDDS)。通过EFN饱和溶解度筛选辅料。通过拟三元图对MCT油/Solutol HS 15/Labrafil M2125 CS SNEDDS (5/75/20, w/w)进行优化。表征包括液滴大小、PDI、zeta电位、形态和药物赋形剂相容性。通过ph值测量溶解度,通过Franz扩散池测试EFN SNEDDS与EFN悬浮液的渗透性。采用纸盘扩散法测定了对红毛癣菌(Trichophyton rubrum)和墨氏毛癣菌(Trichophyton mentagrophytes)的抑菌活性,用扫描电镜(SEM)检测了菌丝对人指甲的损伤。在室内、加速和应力条件下研究了6个月的稳定性。结果:优化后的SNEDDS形成了小于50 nm的液滴,具有较低的多分散性和良好的ζ电位。在不同的pH值下保持溶解度,累积渗透性比悬浮液增加13.6倍。纸盘试验显示,EFN剂量越低,抑制区越大。人指甲上的扫描电镜显示有明显的菌丝破坏。透射电镜证实了球形纳米乳液滴。FT-IR无新峰,支持相容性。在所有储存条件下,粒径、PDI、zeta电位和药物含量在6个月内保持稳定。结论:10% w/w EFN SNEDDS增强了溶解度、经口渗透性和抗真菌效果,同时保持了强大的稳定性,支持其作为一种无乙醇治疗甲癣的潜力。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Enhanced Efinaconazole Permeation and Activity Against Trichophyton rubrum and Trichophyton mentagrophytes with a Self-Nanoemulsifying Drug Delivery System.

Background: Onychomycosis responds poorly to topical therapy, and efinaconazole (EFN) has low aqueous solubility. Methods: This study aimed to develop a 10% w/w EFN self-nanoemulsifying system (SNEDDS) with improved solubility, permeation, antifungal activity, and stability. Excipients were screened by EFN saturation solubility. An MCT oil/Solutol HS 15/Labrafil M2125 CS SNEDDS (5/75/20, w/w) was optimized via a pseudo-ternary diagram. Characterization included droplet size, PDI, and zeta potential, morphology, and drug-excipient compatibility. Solubility was measured across pH. Permeation of EFN SNEDDS vs. EFN suspension was tested by Franz diffusion cells. Antifungal activity against Trichophyton rubrum and Trichophyton mentagrophytes was assessed by paper-disc diffusion, and hyphal damage on human nails was examined by SEM. Stability was studied for six months under room, accelerated, and stress conditions. Results: The optimized SNEDDS formed sub-50 nm droplets with low polydispersity and favourable zeta potential. Solubility was maintained across pH, and cumulative permeation increased 13.6-fold versus suspension. Paper-disc assays showed larger inhibition zones at lower EFN doses. SEM on human nails revealed marked hyphal destruction. TEM confirmed spherical nanoemulsion droplets. FT-IR showed no new peaks, supporting compatibility. Particle size, PDI, zeta potential, and drug content remained stable over six months under all storage conditions. Conclusions: A 10% w/w EFN SNEDDS enhanced solubility, transungual permeation, and antifungal efficacy while maintaining robust stability, supporting its potential as an ethanol-free therapy for onychomycosis.

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来源期刊
Pharmaceutics
Pharmaceutics Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
CiteScore
7.90
自引率
11.10%
发文量
2379
审稿时长
16.41 days
期刊介绍: Pharmaceutics (ISSN 1999-4923) is an open access journal which provides an advanced forum for the science and technology of pharmaceutics and biopharmaceutics. It publishes reviews, regular research papers, communications,  and short notes. Covered topics include pharmacokinetics, toxicokinetics, pharmacodynamics, pharmacogenetics and pharmacogenomics, and pharmaceutical formulation. Our aim is to encourage scientists to publish their experimental and theoretical details in as much detail as possible. There is no restriction on the length of the papers. The full experimental details must be provided so that the results can be reproduced.
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