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. 2013 Oct 1;454(2):775-83.
doi: 10.1016/j.ijpharm.2013.05.017. Epub 2013 May 18.

Budesonide-loaded nanostructured lipid carriers reduce inflammation in murine DSS-induced colitis

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Budesonide-loaded nanostructured lipid carriers reduce inflammation in murine DSS-induced colitis

Ana Beloqui et al. Int J Pharm. .

Abstract

The challenge for the treatment of inflammatory bowel disease (IBD) is the delivery of the drug to the site of inflammation. Because nanoparticles have the ability to accumulate in inflamed regions, the aim of the present study was to evaluate nanostructured lipid carriers (NLCs) as nanoparticulate drug delivery systems for the treatment of IBD. Budesonide (BDS) was chosen as a candidate anti-inflammatory drug. BDS-loaded NLCs (BDS-NLC) produced by high-pressure homogenization had a size of 200 nm and a negative zeta potential. BDS-NLCs reduced the TNF-α secretion by activated macrophages (J774 cells). BDS-NLCs were more active in a murine model of dextran sulfate-induced colitis when compared with Blank-NLCs or a BDS suspension: BDS-NLCs decreased neutrophil infiltration, decreased the levels of the pro-inflammatory cytokines IL-1β and TNF-α in the colon and improved the histological scores of the colons. These data suggest that NLCs could be a promising alternative to polymeric nanoparticles as a targeted drug delivery system for IBD treatment.

Keywords: Budesonide; Colonic delivery; Inflammatory bowel disease; Macrophages; Nanostructured lipid carriers.

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