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

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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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Acknowledgment

The authors are thankful to Unicure Pvt Ltd Noida., India, for providing gift sample of Itraconazole.

Author information

Authors and Affiliations

  1. Department of Pharmaceutics, College of Pharmacy, Jouf University, Aljouf, Saudi Arabia

    Ameeduzzafar & Nabil K Alruwaili

  2. Department of Pharmaceutics, School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi, India

    Mohd Qumber & Asgar Ali

  3. Department of Pharmaceutical Chemistry, College of Pharmacy, Jouf University, Aljouf, Saudi Arabia

    Syed Nasir Abbas Bukhari

  4. Department of Pharmacology, College of Pharmacy, Jouf University, Aljouf, Saudi Arabia

    Khalid Saad Alharbi & Muhammad Afzal

  5. Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia

    Syed Sarim Imam

  6. Department of Pharmacology, College of Pharmacy, Northern Border University, Rafha, Saudi Arabia

    Bader Alsuwayt

  7. Department of Pharmaceutics, College of Pharmacy, Northern Border University, Rafha, Saudi Arabia

    Ali Mujtaba

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  1. Ameeduzzafar
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  2. Mohd Qumber
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Correspondence to Ameeduzzafar.

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Ameeduzzafar, Qumber, M., Alruwaili, N.K. et al. BBD-Based Development of Itraconazole Loaded Nanostructured Lipid Carrier for Topical Delivery: In Vitro Evaluation and Antimicrobial Assessment. J Pharm Innov 16, 85–98 (2021). https://doi.org/10.1007/s12247-019-09420-5

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  • DOI: https://doi.org/10.1007/s12247-019-09420-5

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