BBD-Based Development of Itraconazole Loaded Nanostructured Lipid Carrier for Topical Delivery: In Vitro Evaluation and Antimicrobial Assessment

Objectives The present study was aimed to develop itraconazole (ITZL)-loaded NLC for the treatment of fungal infection. Methods The formulation was prepared and optimized by the hot homogenization method and Box-Behnken statistical design. The total lipid ratio (A), surfactant (B), and homogenization cycle (C) were selected as independent variables, and the effects of variables were evaluated on particle size (R-1), entrapment efficiency (R-2), and drug release in 12 h (R-3). Results The optimized formulation ITZLNLCopt showed particle size (147.31 +/- 1.43 nm) high entrapment efficiency (86.36 +/- 0.83%) and drug release (77.23 +/- 3.33 %). The formulation ITZLNLCopt converted to carbopol (1% w/v) based gel (ITZLNLCopt gel) and showed good consistency and spreadability. The formulation ITZLNLCopt gel showed higher drug release (88.43 +/- 2.54 % up to 24 h) and flux (2.46 fold) than control gel. The zone of inhibition results showed 2.6 and 2.36 fold higher inhibition (P< 0.05) than control gel (ITZL gel) againstCandida albicansandAspergillus fumigatus. Conclusions It could be concluded that ITZLNLC gel as a potential alternative for the treatment of topical fungal infection after clinical study in the future.

Automated summary

The study successfully developed itraconazole-loaded nanostructured lipid carriers and further formulated them into a gel, showing good consistency and spreadability. The nanostructured lipid carrier gel exhibited higher drug release and inhibition effect against fungal infections compared to the control group.