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

Ameeduzzafar, Mohd Qumber, Nabil K. Alruwaili, Syed Nasir Abbas Bukhari, Khalid Saad Alharbi, Syed Sarim Imam, Muhammad Afzal, Bader Alsuwayt, Ali Mujtaba, Asgar Ali

Research output: Contribution to journalArticle

Abstract

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 (R1), entrapment efficiency (R2), and drug release in 12 h (R3). 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.

Original languageEnglish
JournalJournal of Pharmaceutical Innovation
DOIs
Publication statusAccepted/In press - 1 Jan 2020

Fingerprint

Itraconazole
Gels
Lipids
Mycoses
Particle Size
Aspergillus fumigatus
In Vitro Techniques
Candida albicans
Surface-Active Agents
Drug Liberation

Keywords

  • Antimicrobial activity
  • Itraconazole
  • Nanolipid carrier
  • Skin irritation study
  • Skin permeation

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Drug Discovery

Cite this

BBD-Based Development of Itraconazole Loaded Nanostructured Lipid Carrier for Topical Delivery : In Vitro Evaluation and Antimicrobial Assessment. / Ameeduzzafar; Qumber, Mohd; Alruwaili, Nabil K.; Bukhari, Syed Nasir Abbas; Alharbi, Khalid Saad; Imam, Syed Sarim; Afzal, Muhammad; Alsuwayt, Bader; Mujtaba, Ali; Ali, Asgar.

In: Journal of Pharmaceutical Innovation, 01.01.2020.

Research output: Contribution to journalArticle

Ameeduzzafar ; Qumber, Mohd ; Alruwaili, Nabil K. ; Bukhari, Syed Nasir Abbas ; Alharbi, Khalid Saad ; Imam, Syed Sarim ; Afzal, Muhammad ; Alsuwayt, Bader ; Mujtaba, Ali ; Ali, Asgar. / BBD-Based Development of Itraconazole Loaded Nanostructured Lipid Carrier for Topical Delivery : In Vitro Evaluation and Antimicrobial Assessment. In: Journal of Pharmaceutical Innovation. 2020.
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abstract = "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 (R1), entrapment efficiency (R2), and drug release in 12 h (R3). 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.",
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AU - Alruwaili, Nabil K.

AU - Bukhari, Syed Nasir Abbas

AU - Alharbi, Khalid Saad

AU - Imam, Syed Sarim

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AU - Alsuwayt, Bader

AU - Mujtaba, Ali

AU - Ali, Asgar

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AB - 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 (R1), entrapment efficiency (R2), and drug release in 12 h (R3). 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.

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