2026-04-14T04:35:50Zhttps://recercat.cat/oai/request

oai:recercat.cat:2445/2183042025-11-19T10:41:32Zcom_2072_1057col_2072_478815col_2072_478917

Formulation Design and Optimization for the Improvement of Nystatin-Loaded Lipid Intravenous Emulsion Marín-Quintero, D. Fernández Campos, Francisco Calpena Campmany, Ana Cristina Montes López, María Jesús Clares Naveros, Beatriz Pozo Carrascosa, Alfonso del Lípids Emulsions Lipids Emulsions ABSTRACT: Nystatin (NYS) is a polyene macrolide with broad antifungal spectrum restricted to topical use owing to its toxicity upon systemic administration. The aims of thiswork were the design, development, and optimization ofNYS-loaded lipid emulsion for intravenous administration. A closed circuit system was designed to apply ultrasound during the elaboration of the lipid intravenous emulsions (LIEs). Additionally, a comparison with the commercially available Intralipid R 20% was also performed.Manufacturing conditions were optimized by factorial design. Formulations were evaluated in terms of physicochemical parameters, stability, release profile, and antimicrobial activity. The average droplet size, polydispersity index, zeta-potential, pH, and volume distribution values ranged between 192.5 and 143.0 nm, 0.170 and 0.135, −46 and −44 mV, 7.11 and 7.53, 580 and 670 nm, respectively. The selected NYS-loaded LIE (NYS-LIE54) consisted of soybean oil (30%), soybean lecithin (2%), solutol HSR 15 (4%), and glycerol (2.25%) was stable for at least 60 days. In vitro drug release studies of this formulation suggested a sustained-release profile. Equally, NYS-LIE54 showed the best antimicrobial activity being higher than the free drug. Thus, it could be a promising drug delivery system to treat systemic fungal infections. C 2013 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci Keywords: drug design; nystatin; lipids; emulsion; injectables; surfactants; candida; aspergillus; mathematical model 2025-01-31T09:44:32Z 2025-01-31T09:44:32Z 2013-11-22 2025-01-31T09:44:32Z info:eu-repo/semantics/article info:eu-repo/semantics/acceptedVersion Versió postprint del document publicat a: Journal of Pharmaceutical Sciences, 2013, vol. 102, num.11, p. 4015-4023 (c) The American Pharmacists Association, 2013 info:eu-repo/semantics/openAccess Wiley Articles publicats en revistes (Farmàcia, Tecnologia Farmacèutica i Fisicoquímica)