Fungal infection of the skin is one of the most common dermatological diseases in the world. Gel formulations are among the most suitable dosage forms for topical use to treat cutaneous infection. Nanotechnology is a promising approach to penetrate the deeper skin layers and enhance permeability of itraconazole (ITZ) through the stratum corneum. ITZ-loaded nanoparticles (ITZ NPs) were fabricated using the evaporation emulsion method, followed by incorporation of NPs into gel using Carbopol 934 as the gel-forming excipient. The physical properties, in vitro release, ex vivo permeation studies, and antifungal activity of ITZ NP gel were characterized. ITZ NPs were almost spherical in shape with colloidal sizes in the range of 200 nm. The drug encapsulation efficiency was %. ITZ NP gel demonstrated a sustained ex vivo permeation of ITZ over 24 h through excised rat skin and a higher drug penetrating capacity than that of a gel containing ITZ-saturated suspension. The in vitro antifungal activity of the ITZ-loaded NP incorporated gel was better than that of ITZ dispersion. Incorporation of the ITZ-loaded nanosystem into gel has the potential to enhance antifungal activity through transdermal drug delivery.

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依他康唑负载的聚合物纳米颗粒皮肤凝胶增强抗真菌功效的开发

皮肤的真菌感染是世界上最常见的皮肤病。凝胶制剂是最适合用于局部治疗皮肤感染的剂型。纳米技术是一种有前景的方法，可以穿透更深的皮肤层，并提高伊曲康唑（ITZ）通过角质层的渗透性。使用蒸发乳液法制备负载ITZ的纳米颗粒（ITZ NPs），然后使用Carbopol 934作为形成凝胶的赋形剂将NPs掺入凝胶中。物理性质，体外释放，离体表征了ITZ NP凝胶的渗透研究和抗真菌活性。ITZ NP的形状几乎为球形，胶体大小在200 nm范围内。药物包封率为％。ITZ NP凝胶显示，经过离体的大鼠皮肤，ITZ可以在24小时内持续离体渗透，并且比包含ITZ饱和悬浮液的凝胶具有更高的药物穿透能力。在体外的ITZ加载NP掺入凝胶的抗真菌活性比ITZ分散体更好。将ITZ负载的纳米系统并入凝胶中具有通过透皮药物递送增强抗真菌活性的潜力。