LIPID NANOEMULSION-BASED LIQUISOLID COMPACT TABLETS FOR ORAL DELIVERY OF CLOTRIMAZOLE: FABRICATION STRATEGIES, CHARACTERIZATIONS, ANTIMYCOTIC AND TOXICOLOGICAL EVALUATIONS | ||||
Bulletin of Pharmaceutical Sciences Assiut University | ||||
Volume 45, Issue 2, December 2022, Page 533-564 PDF (2.41 MB) | ||||
Document Type: Original Article | ||||
DOI: 10.21608/bfsa.2022.271487 | ||||
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Authors | ||||
Chukwuebuka Emmanuel Umeyor 1; Ifeyinwa Ezechukwu1; Chiamaka Okafor1; Marksaviour Ibe1; Tochukwu Okeke1; Ngozi Nebolisa 1; Emmanuel Uronnachi1; Anthony Attama2 | ||||
1Nanomedicines and Drug Delivery Research Group, Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Nnamdi Azikiwe University, Awka, 422001, Anambra State, Nigeria | ||||
2Drug Delivery and Nanomedicine Research Group, Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of Nigeria, Nsukka, 410001, Enugu State, Nigeria | ||||
Abstract | ||||
This work aims to fabricate liquisolid compact tablets incorporating clotrimazole (CLOT)-loaded lipid nanoemulsions (LNE) for oral treatment of systemic fungal infections. Nanoemulsion was characterized for droplet size, rendered into free-flowing granules and compressed into liquisolid compact tablets, and evaluated using pharmacopoeial and non-pharmacopoeial methods. In-vitro and in vivo antifungal, stability and toxicological tests of the tablets were evaluated. LNE was nanosized (66.7 ± 5.7 – 121.6 ± 3.2 nm). Liquisolid tablets were stable, non-toxic, had uniform weight (341.4 ± 1.2 – 346.7 ± 0.8 mg), drug content uniformity (85.2 ± 0.1 – 99.8 ± 0.2 %), and had excellent disintegration (2.96 ± 0.8 – 5.88 ± 1.3 min), and controlled release property. In-vitro and in vivo antifungal evaluations revealed improved antimycotic activity of CLOT. The results highlight that CLOT-LNE liquisolid compact tablets is a promising carrier system with improved oral utility for the treatment of systemic fungal infections. | ||||
Keywords | ||||
Clotrimazole; Lipid nanoemulsion; Liquisolid; Systemic mycoses; Candida albicans; Oral delivery | ||||
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