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Delivery of tacrolimus with cationic lipid-assisted nanoparticles for ulcerative colitis therapy

Abstract

Oral drug delivery with nanoparticles has demonstrated great potential for drugs with poor bioavailability. Efficient delivery is possible by overcoming both the mucus and epithelial barrier of the gastrointestinal tract (GIT). Cationic lipid-assisted nanoparticles (CLANs) which are composed of amphiphilic block copolymers and cationic lipid have been well studied and exhibit advantages on drug delivery. In this study, CLANs prepared by poly(ethylene glycol)-block-poly(lactic acid) (PEG-b-PLA) and 1,2-dioleoyl-3-trimethylammonium-propanechloride (DOTAP) or N,N-bis(2-hydroxyethyl)-N-methyl-N-(2-cholesteryloxycarbonyl aminoethyl) ammoni-umbromide (BHEM-Chol) were used for oral delivery of tacrolimus (FK506) for ulcerative colitis treatment. The sizes of these nanoparticles are around 110 nm and the zeta-potentials are at 35 mV. Those nanoparticles maintained their size in buffers of pH 1.2 and 6.8, and slowly release the encapsulated drug. CLANs can be well accumulated in colon and transport through epithelium in colitis model induced by dextran sulfate sodium salt (DSS) leading to attenuation of DSS-induced colitis.

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Publication details

The article was received on 27 Apr 2018, accepted on 13 May 2018 and first published on 14 May 2018


Article type: Paper
DOI: 10.1039/C8BM00463C
Citation: Biomater. Sci., 2018, Accepted Manuscript
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    Delivery of tacrolimus with cationic lipid-assisted nanoparticles for ulcerative colitis therapy

    J. Wang, Y. Gan, S. Iqbal, W. Jiang, Y. Yuan and J. Wang, Biomater. Sci., 2018, Accepted Manuscript , DOI: 10.1039/C8BM00463C

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