Development of Itraconazole-Loaded Polymeric Nanoparticle Dermal Gel for Enhanced Antifungal Efficacy

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 98.79 +- 1.24 %. 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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Article Information: Hoang Nhan Ho, Thien Giap Le, Thi Thanh Tuyen Dao, Thi Ha Le, Thi Thanh Hai Dinh, Dang Hoa Nguyen, Trinh Cong Tran, and Chien Ngoc Nguyen. Journal of Nanomaterials, 2020. https://doi.org/10.1155/2020/8894541

Materials: All chemicals were used without further purification and obtained from the following commercial sources: ITZ (Yashica Pharmaceuticals Private Limited, Maharashtra, India), EC (Shanghai Colorcon Coating Technology Ltd., Shanghai, China), dichloromethane (Xilong Scientific Co., Ltd., Guangdong, China), polyvinyl alcohol (Kuraray Asia Pacific Pte. Ltd., Singapore), polysorbate 80 (Tween 80; Duksan Chemical Co., Ansan, South Korea), propylene glycol (PG, Zhejiang Kehong Chemical Co., Zhejiang, China), and Carbopol 934 (CBP 934; Lubrizol Corp., Wickliffe, Ohio, USA). Methanol was of high-performance liquid chromatography (HPLC) grade. Other chemicals were of analytical grade.