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Delivery system for budesonide based on lipid-DNA.

Liu, Yun
; 
Bos, I Sophie T
; 
Oenema, Tjitske A
; 
Meurs, Herman
; 
Maarsingh, Harm
; 
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2018-09-01
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Abstract
Budesonide is a hydrophobic glucocorticoid with high anti-inflammatory activity for the treatment of asthma, inflammatory bowel disease and rheumatoid arthritis. A micellar drug-delivery system based on lipid-DNA may provide a strategy to maximize its drug efficacy and reduce adverse effects. In this work, we report the use of lipid-DNAA (UU11mer), featuring two hydrophobic alkyl chains and forming micelles at a comparatively low critical micelle concentration, to render budesonide water-soluble with a high loading capacity (LC). The inhibition of interleukin-8 (IL-8) release shows that the new delivery system retains the inhibitory activity in cell-based assays. In conclusion, this research provides a novel approach to formulate and administer budesonide in a non-invasive manner, which dramatically improves its water-solubility while retaining its bioavailability.
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Affiliation
HIPS, Helmholtz-Institut für pharmazeutische Forschung Saarland, Universitätscampus 8.1, 66123 Saarbrücken, Germany.
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http://hdl.handle.net/10033/621489
DOI
10.1016/j.ejpb.2018.06.012
PubMed ID
29908939
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1873-3441
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Attribution-NonCommercial-ShareAlike 3.0 United States
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publications of the research group drug design and optimization(HIPS]DDOP)