LIPID NANOEMULSION-BASED LIQUISOLID COMPACT TABLETS FOR ORAL DELIVERY OF CLOTRIMAZOLE: FABRICATION STRATEGIES, CHARACTERIZATIONS, ANTIMYCOTIC AND TOXICOLOGICAL EVALUATIONS

Umeyor, Chukwuebuka Emmanuel; Ezechukwu, Ifeyinwa; Okafor, Chiamaka; Ibe, Marksaviour; Okeke, Tochukwu; Nebolisa, Ngozi; Uronnachi, Emmanuel; Attama, Anthony

doi:10.21608/bfsa.2022.271487

LIPID NANOEMULSION-BASED LIQUISOLID COMPACT TABLETS FOR ORAL DELIVERY OF CLOTRIMAZOLE: FABRICATION STRATEGIES, CHARACTERIZATIONS, ANTIMYCOTIC AND TOXICOLOGICAL EVALUATIONS

Document Type : Original Article

Authors

¹ Nanomedicines and Drug Delivery Research Group, Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Nnamdi Azikiwe University, Awka, 422001, Anambra State, Nigeria

² Drug Delivery and Nanomedicine Research Group, Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of Nigeria, Nsukka, 410001, Enugu State, Nigeria

10.21608/bfsa.2022.271487

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.

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