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Heba A Abou-Taleb,1 Rasha A Khallaf,2 Jelan A Abdel-Aleem3 1Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Nahda University (NUB), Beni Suef, Egypt; 2Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Beni-Suef University, Beni Suef, Egypt; 3Department of Industrial Pharmacy, Faculty of Pharmacy, Assiut University, Assiut, Egypt Objective: One of the greatest challenges drug formulation is facing is poor bioavailability via oral route. In this regard, nasal drug delivery has been commonly used as an alternative route to improve drug bioavailability. Nefopam hydrochloride (NF) is an analgesic drug that suffers from poor bioavailability due to extensive metabolism in liver. Accordingly, the goal of the present study was to improve NF bioavailability via niosomal-based formulation designed for intranasal delivery.Materials and methods: Vesicles were developed by mixing surfactants (Span 20, Span 40, Span 80, and Span 85) at four molar ratios of 1:1, 1:2, 1:3, and 1:4 of cholesterol to surfactant. Entrapment efficiency, particle size, zeta potential, release percentage, ex-vivo permeation parameters, and niosomes’ stability were determined. Also, the pharmacokinetic parameters of the optimized formula in in-situ gel base were measured in rats.Results: Niosomes showed entrapment efficiency >80%, particle size |
