油酸囊泡是硝酸益康唑透皮给药的一种新方法:在 Wistar 大鼠体内进行开发、表征和体内评估。

Q3 Medicine
Shivani Verma, Puneet Utreja
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引用次数: 0

摘要

背景:皮肤念珠菌病是一种深层皮肤真菌感染,最常见于免疫力低下的患者。治疗这种真菌感染的传统方法是使用凝胶和药膏等各种制剂,但这些制剂都有不同的副作用,而且疗效甚微。因此,有必要开发一种新型载体系统来治疗这种深层皮肤真菌感染。硝酸益康唑是治疗皮肤念珠菌病最广泛使用的抗真菌药物,因此,在本研究工作中,我们开发并评估了通过透皮途径治疗皮肤念珠菌病的硝酸益康唑负载油酸囊泡:方法:通过薄膜水合法制备了硝酸益康唑负载油酸囊泡,并对药物包被、囊泡大小、ZETA电位、多分散指数(PDI)、傅立叶变换红外光谱(FT-IR)、差示扫描量热仪(DSC)、X射线衍射(XRD)分析进行了表征。此外,还对油酸囊状凝胶在 Wistar 大鼠体内的体外皮肤渗透/滞留以及体内和体外抗真菌活性进行了评估:结果:负载硝酸益康唑的油酸囊泡显示出较高的药物包封率(74.76 ± 3.0%)、可接受的尺寸(373.4 ± 2.9 nm)和胶体特性(PDI = 0.231 ± 0.078,zeta电位 = -13.27 ± 0.80 mV)。与市场上销售的硝酸益康唑乳膏(EcodermR)相比,油酸囊状凝胶具有较高的皮肤渗透性(透皮通量 = 61.98 ± 2.45 μg/cm2/h)、皮肤保留率(35.90 ± 2.06%)、体外和体内抗真菌活性,并可长期使用(4 天):开发的硝酸益康唑负载油酸囊泡可有效用于治疗皮肤念珠菌病,在提高疗效的同时将硝酸益康唑的副作用降至最低。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Oleic Acid Vesicles as a new Approach for Transdermal Delivery of Econazole Nitrate: Development, Characterization, and In-vivo Evaluation in Wistar rats.

Background: Cutaneous candidiasis is a deep-seated skin fungal infection that is most commonly observed in immunocompromised patients. This fungal infection is conventionally treated with various formulations like gels and creams which are having different side effects and least therapeutic efficacy. Hence, it becomes necessary to develop a novel carrier system for the treatment of this deep-seated skin fungal infection. Econazole nitrate is the most widely used antifungal for the treatment of cutaneous candidiasis, therefore, in present research work we developed and evaluated econazole nitrate loaded oleic acid vesicles for treatment of cutaneous candidiasis through transdermal route.

Methods: Econazole nitrate loaded oleic acid vesicles were prepared by thin-film hydration and characterized for drug entrapment, vesicle size, zeta potential, polydispersity index (PDI), Fourier Transform-infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), X-ray diffraction (XRD) analysis. Furthermore, the oleic acid vesicular gel was evaluated for ex-vivo skin permeation/retention and in-vitro and in-vivo antifungal activity in Wistar rats.

Results: Econazole nitrate loaded oleic acid vesicles showed high encapsulation of drug (74.76 ± 3.0%), acceptable size (373.4 ± 2.9 nm), and colloidal characteristics (PDI = 0.231 ± 0.078, zeta potential = -13.27 ± 0.80 mV). The oleic acid vesicular gel showed high skin permeation (Transdermal flux = 61.98 ± 2.45 μg/cm2/h), skin retention (35.90 ± 2.06%), in-vitro, and in-vivo antifungal activity compared to marketed cream (EcodermR) of econazole nitrate for a prolonged period of time (4 days).

Conclusion: Developed econazole nitrate loaded oleic acid vesicles could be used effectively in the treatment of cutaneous candidiasis with minimization of side effects of econazole nitrate with increased therapeutic efficacy.

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来源期刊
Recent patents on anti-infective drug discovery
Recent patents on anti-infective drug discovery Medicine-Pharmacology (medical)
CiteScore
2.40
自引率
0.00%
发文量
1
期刊介绍: Recent Patents on Anti-Infective Drug Discovery publishes review articles on recent patents in the field of anti-infective drug discovery e.g. novel bioactive compounds, analogs & targets. A selection of important and recent patents on anti-infective drug discovery is also included in the journal. The journal is essential reading for all researchers involved in anti-infective drug design and discovery.
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