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用于真菌感染的载有硝酸奥昔康唑的纳米结构脂质载体凝胶的皮肤靶向性

Skin Targeting of Oxiconazole Nitrate Loaded Nanostructured Lipid- Carrier Gel for Fungal Infections.

作者信息

Ranpise Hemantkumar A, Gujar Kishor N, Mathure Dyandevi, Satpute Pooja P, Awasthi Rajendra, Dua Kamal, Madan Jyotsana R

机构信息

Department of Pharmaceutics, Sinhgad College of Pharmacy, Savitribai Phule Pune University, Pune, Maharashtra, India.

Department of Pharmaceutics, Smt. Kashibai Navale College of Pharmacy, Savitribai Phule Pune University, Pune, Maharashtra, India.

出版信息

Pharm Nanotechnol. 2018;6(3):192-200. doi: 10.2174/2211738506666180913125918.

Abstract

BACKGROUND

The progression of fungal infections can be rapid and serious due to compromising with immune function. They may cause liver damage, affect estrogen levels or may cause allergic reactions. Oxiconazole nitrate (OXZN) is a broad spectrum commonly used antifungal drug. It acts by erogosterol biosynthesis inhibition, which causes lysis of the fungal cell membrane because of changes in both membrane integrity and fluidity and direct membrane damage of fungal cells. However, its poor water solubility and short half-life (3-5 h) limit its applications.

OBJECTIVE

This study aimed to develop and evaluate OXZN-loaded nanostructured lipid carrier (NLC) to improve its solubility and prolong its release for the treatment of fungal infection via topical administration.

METHOD

OXZN-NLC was prepared by ultrasonication method using 32 full factorial design. Glyceryl monostearate (GMS) (X1) and oleic acid (X2) were used as independent variables and particle size and percentage entrapment efficiency (% EE) as dependent variables. The OXZN-NLCs were characterized for particle size, particle morphology and entrapment efficiency.

RESULTS

The mean diameter of optimized OXZN-NLCs was found to be 124 ± 2 nm. Spherical shape and size were confirmed using scanning electron microscopy (SEM). Skin deposition study showed about 82.74% deposition as compared with the marketed formulation that showed 68.42% deposition. The developed NLCs show a sustained release pattern and high drug disposition in the infected area.

CONCLUSION

OXZN-NLC could be a potential alternative for the treatment of topical fungal infection after clinical evaluation in near future.

摘要

背景

由于免疫功能受损,真菌感染的进展可能迅速且严重。它们可能导致肝损伤、影响雌激素水平或引起过敏反应。硝酸奥昔康唑(OXZN)是一种常用的广谱抗真菌药物。它通过抑制麦角甾醇生物合成起作用,由于膜完整性和流动性的变化以及真菌细胞膜的直接损伤,导致真菌细胞膜溶解。然而,其水溶性差和半衰期短(3 - 5小时)限制了其应用。

目的

本研究旨在开发和评估负载OXZN的纳米结构脂质载体(NLC),以提高其溶解度并延长其释放时间,通过局部给药治疗真菌感染。

方法

采用32全因子设计,通过超声法制备OXZN - NLC。以单硬脂酸甘油酯(GMS)(X1)和油酸(X2)作为自变量,粒径和包封率(%EE)作为因变量。对OXZN - NLC进行粒径、颗粒形态和包封率表征。

结果

优化后的OXZN - NLC平均直径为124±2nm。通过扫描电子显微镜(SEM)确认了球形形状和尺寸。皮肤沉积研究表明,与市售制剂68.42%的沉积率相比,沉积率约为82.74%。所制备的NLC显示出持续释放模式以及在感染区域的高药物分布。

结论

在不久的将来进行临床评估后,OXZN - NLC可能成为治疗局部真菌感染的潜在替代品。

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