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 homogenizatio...

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Veröffentlicht in:Journal of pharmaceutical innovation 2021-03, Vol.16 (1), p.85-98
Hauptverfasser: Ameeduzzafar, Qumber, Mohd, Alruwaili, Nabil K, Bukhari, Syed Nasir Abbas, Alharbi, Khalid Saad, Imam, Syed Sarim, Afzal, Muhammad, Alsuwayt, Bader, Mujtaba, Ali, Ali, Asgar
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Sprache:eng
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Zusammenfassung: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) against Candida albicans and Aspergillus 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.
ISSN:1872-5120
1939-8042
DOI:10.1007/s12247-019-09420-5