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2013-11-22

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Si us plau utilitzeu sempre aquest identificador per citar o enllaçar aquest document: https://hdl.handle.net/2445/218304

Formulation Design and Optimization for the Improvement of Nystatin-Loaded Lipid Intravenous Emulsion

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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

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Lípids, Emulsions

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Lipids, Emulsions

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Articles publicats en revistes (Farmàcia, Tecnologia Farmacèutica i Fisicoquímica)

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MARÍN-QUINTERO, D., et al. Formulation Design and Optimization for the Improvement of Nystatin-Loaded Lipid Intravenous Emulsion. Journal of Pharmaceutical Sciences. 2013. Vol. 102, num. 11, pags. 4015-4023. ISSN 0022-3549. [consulted: 16 of August of 2026]. Available at: https://hdl.handle.net/2445/218304

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