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Solid lipid nanoparticles (SLN) as carriers for the topical delivery of econazole nitrate: in-vitro characterization, ex-vivo and in-vivo studies

Sanna, Vanna Annunziata and Gavini, Elisabetta and Cossu, Massimo and Rassu, Giovanna and Giunchedi, Paolo (2007) Solid lipid nanoparticles (SLN) as carriers for the topical delivery of econazole nitrate: in-vitro characterization, ex-vivo and in-vivo studies. Journal of Pharmacy and Pharmacology, Vol. 59 (8), p. 1057-1064. ISSN 0022-3573. eISSN 2042-7158. Article.

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DOI: 10.1211/jpp.59.8.0002

Abstract

Solid lipid nanoparticles (SLN) designed for topical administration of econazole nitrate (ECN), were prepared by o/w high-shear homogenization method using different ratios of lipid and drug (5:1 and 10:1). SLN were characterized in terms of particle size, morphology, encapsulation efficiency and crystalline structure. After incorporation of SLN into hydrogels, rheological measurements were performed, and ex-vivo drug permeation tests were carried out using porcine stratum corneum (SC). In-vivo study of percutaneous absorption of ECN as a function of application time and composition of gels was carried out by tape-stripping technique. Penetration tests of the drug from a conventional gel were performed as comparison. High-shear homogenization method resulted in a good technique for preparation of ECN-loaded SLN. Particles had a mean diameter of about 150 nm and a regular shape and smooth surface. The encapsulation efficiency values were about 100%. Ex-vivo tests showed that SLN were able to control the drug release through the SC; the release rate depended upon the lipid content on the nanoparticles. In-vivo studies demonstrated that SLN promoted a rapid penetration of ECN through the SC after 1 h and improved the diffusion of the drug in the deeper skin layers after 3 h of application compared with the reference gel.

Item Type:Article
ID Code:4804
Status:Published
Refereed:Yes
Uncontrolled Keywords:Solid lipid nanoparticles (SLN), Econazole nitrate (ECN), high-shear homogenization, Skin
Subjects:Area 03 - Scienze chimiche > CHIM/09 Farmaceutico tecnologico applicativo
Divisions:001 Università di Sassari > 01 Dipartimenti > Scienze del farmaco
Publisher:Wiley
ISSN:0022-3573
eISSN:2042-7158
Copyright Holders:© 2007 The Authors
Deposited On:12 Nov 2010 10:11

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