Ketoconazole-Loaded Cationic Nanoemulsion: -- Evaluations to Control Cutaneous Fungal Infections.

ACS Omega

Department of Pharmacy, Eugene Applebaum, College of Pharmacy and Health Sciences, Wayne State University, Detroit, Michigan 48201, United States.

Published: June 2022

An attempt has been made to optimize ketoconazole (KTZ)-loaded cationic nanoemulsion for topical delivery followed by , , and evaluations. Central composite design suggested a total of 13 outcomes at 3 factors and 2 levels against 6 responses. Formulations were characterized for globular size, polydispersity index, pH, ζ potential, % entrapment efficiency (% EE), and drug content. Moreover, the optimized KTZ-CNM13 was compared against drug suspension (KTZ-SUS), commercial cream, and anionic nanoemulsion for drug release, permeation, hemolysis, antifungal assay, dermal irritancy, and long-term stability. KTZ-CNM13 was found to have a low size (239 nm), an optimal ζ potential (+22.7 mV), a high % EE (89.1%), a spherical shape, a high drug content (98.9%), and a high numerical desirability value (1.0). drug release behavior of KTZ from KTZ-CNM13 was 7.54- and 1.71-folds higher than those of KTZ-ANM13 and KTZ-SUS, respectively, at 24 h. The permeation rate values were ordered as KTZ-CNM13 > KTZ-ANM13 > KTZ-MKT > KTZ-SUP due to various studied factors. High values of zone of inhibition for KTZ-CNM13 were observed against , , and as compared to KTZ-SUS. hemolysis and irritation studied confirmed the safety concern of the nanoemulsion at the explored composition. Long-term stability result revealed a stable product at the explored temperature for a year. Conclusively, cationic nanoemulsion is a promising approach to deliver KTZ for high permeation and therapeutic efficacy.

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Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC9201893PMC
http://dx.doi.org/10.1021/acsomega.2c02219DOI Listing

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