Ethyl cellulose-based in-situ film of itraconazole for enhanced treatment of fungal infections.

IF 1 Q4 PHARMACOLOGY & PHARMACY

Annales pharmaceutiques francaises Pub Date : 2025-04-17 DOI:10.1016/j.pharma.2025.04.002

Lutfi Chabib, Yulianto, Putri Wulandari Resky Ananda, Rifka Nurul Utami, Maria Mir, Diany Elim, Andi Maqhfirah Nurul Fitri, Hilman Syamami Zaman, Anugerah Yaumil Ramadhani Aziz, Nurul Fauziah, Latifah Rahman, M Pandoman Febrian, Andi Dian Permana

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引用次数: 0

Abstract

Objectives: Fungal infections represent a significant global health challenge, requiring effective treatments to prevent complications and improve patient outcomes. This study aimed to develop an in-situ film-forming system (IFFS) for transcutaneous delivery of itraconazole (ITZ) as an alternative to oral administration, addressing issues such as low bioavailability, reduced efficacy, and potential side effects.

Materials and methods: The IFFS was formulated using ethyl cellulose as the primary polymer, PEG 400 as a plasticizer, and a eutectic mixture of menthol and camphor as penetration enhancers. The system was characterized for viscosity, pH, drying time, water vapor permeability, bioadhesion, and physicochemical interactions (DSC and FTIR). Ex vivo skin permeation and retention studies were conducted using Franz diffusion cells, and antifungal efficacy was tested on an ex vivo Candida albicans infection model. Skin integrity and hemolysis tests were performed to evaluate safety.

Results: The IFFS exhibited desirable physicochemical properties, with increased polymer concentrations enhancing skin retention and bioadhesive strength while reducing permeation rates. Ex vivo studies showed sustained ITZ release and enhanced skin retention. The antifungal activity test demonstrated complete eradication of Candida albicans within 48hours. Safety assessments confirmed no skin irritation or toxicity.

Conclusion: The developed IFFS provides a safe and effective transcutaneous delivery system for ITZ. This innovative approach enhances antifungal efficacy, improves skin retention, and offers a promising alternative to oral administration, minimizing systemic side effects.

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乙基纤维素基伊曲康唑原位膜对真菌感染的强化治疗。

目的：真菌感染是一个重大的全球健康挑战，需要有效的治疗来预防并发症和改善患者的预后。本研究旨在开发一种原位成膜系统（IFFS），用于经皮给药伊曲康唑（ITZ），作为口服给药的替代方案，解决伊曲康唑生物利用度低、疗效降低和潜在副作用等问题。材料和方法：以乙基纤维素为主要聚合物，PEG 400为增塑剂，薄荷醇和樟脑的共晶混合物为渗透增强剂配制IFFS。对该体系进行了粘度、pH、干燥时间、水蒸气渗透性、生物粘附性和物理化学相互作用（DSC和FTIR）的表征。采用Franz扩散细胞进行体外皮肤渗透和滞留研究，并在体外白色念珠菌感染模型上检测抗真菌效果。进行皮肤完整性和溶血试验来评估安全性。结果：IFFS表现出理想的物理化学性质，聚合物浓度的增加增强了皮肤潴留和生物粘附强度，同时降低了渗透速率。体外研究显示持续的ITZ释放和增强的皮肤保留率。抗真菌活性试验显示在48小时内完全根除白色念珠菌。安全评估证实无皮肤刺激或毒性。结论：所研制的IFFS是一种安全有效的经皮给药系统。这种创新的方法增强了抗真菌功效，改善了皮肤潴留，并提供了口服给药的有希望的替代方案，最大限度地减少了全身副作用。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Annales pharmaceutiques francaises PHARMACOLOGY & PHARMACY-

CiteScore

1.70

自引率

7.70%

发文量

期刊介绍： This journal proposes a scientific information validated and indexed to be informed about the last research works in all the domains interesting the pharmacy. The original works, general reviews, the focusing, the brief notes, subjected by the best academics and the professionals, propose a synthetic approach of the last progress accomplished in the concerned sectors. The thematic Sessions and the – life of the Academy – resume the communications which, presented in front of the national Academy of pharmacy, are in the heart of the current events.