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

• DOI: 10.1007/s12247-019-09420-5
• Publication Date: 2020-01-06T09:04:04Z
• Authors: Ameeduzzafar; Mohd Qumber; Nabil K Alruwaili; Syed Nasir Abbas ...; Khalid Saad Alharbi; Syed Sarim Imam; Muhammad Afzal; Bader Alsuwayt; Ali Mujtaba; Asgar Ali
• Keywords: Box–Behnken design; Homogenization

The present study was aimed to develop itraconazole (ITZL)-loaded NLC for the treatment of fungal infection. 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 (R1), entrapment efficiency (R2), and drug release in 12 h (R3). 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) against Candida albicans and Aspergillus fumigatus. It could be concluded that ITZLNLC gel as a potential alternative for the treatment of topical fungal infection after clinical study in the future.