Development and Optimization of Luliconazole Spanlastics to Augment the Antifungal Activity against Candida albicans

卢立康唑弹性蛋白增强剂的开发和优化,以增强其对白色念珠菌的抗真菌活性

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作者:Nabil A Alhakamy, Mohammed W Al-Rabia, Shadab Md, Alaa Sirwi, Selwan Saud Khayat, Sahar Saad AlOtaibi, Raghad Abkar Hakami, Hadeel Al Sadoun, Basmah Medhat Eldakhakhny, Wesam H Abdulaal, Hibah M Aldawsari, Shaimaa M Badr-Eldin, Mahmoud A Elfaky

Abstract

Luliconazole is a new topical imidazole antifungal drug for the treatment of skin infections. It has low solubility and poor skin penetration which limits its therapeutic applications. In order to improve its therapeutic efficacy, spanlastics nanoformulation was developed and optimized using a combined mixture-process variable design (CMPV). The optimized formulation was converted into a hydrogel formula to enhance skin penetration and increase the efficacy in experimental cutaneous Candida albicans infections in Swiss mice wounds. The optimized formulation was generated at percentages of Span and Tween of 48% and 52%, respectively, and a sonication time of 6.6 min. The software predicted that the proposed formulation would achieve a particle size of 50 nm with a desirability of 0.997. The entrapment of luliconazole within the spanlastics carrier showed significant (p < 0.0001) antifungal efficacy in the immunocompromised Candida-infected Swiss mice without causing any irritation, when compared to the luliconazole treated groups. The microscopic observation showed almost complete removal of the fungal colonies on the skin of the infected animals (0.2 ± 0.05 log CFU), whereas the control animals had 0.2 ± 0.05 log CFU. Therefore, luliconazole spanlastics could be an effective formulation with improved topical delivery for antifungal activity against C. albicans.

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