Format

Send to

Choose Destination
Eur J Pharm Biopharm. 2018 Sep;130:123-127. doi: 10.1016/j.ejpb.2018.06.012. Epub 2018 Jun 14.

Delivery system for budesonide based on lipid-DNA.

Author information

1
School of Pharmacy, Guangdong Medical University, Dongguan 523808, China; Stratingh Institute for Chemistry, University of Groningen, Nijenborgh 7, 9747 AG Groningen, The Netherlands.
2
Department of Molecular Pharmacology, University of Groningen, Antonius Deusinglaan 1, 9713 AV Groningen, The Netherlands.
3
Department of Pharmaceutical Sciences, Lloyd L. Gregory School of Pharmacy, Palm Beach Atlantic University, West Palm Beach, FL, USA.
4
Stratingh Institute for Chemistry, University of Groningen, Nijenborgh 7, 9747 AG Groningen, The Netherlands; Helmholtz Institute for Pharmaceutical Research Saarland (HIPS) - Helmholtz Centre for Infection Research (HZI), Department of Drug Design and Optimization, Campus Building E 8.1, 66123 Saarbr├╝cken, Germany; Department of Pharmacy, Medicinal Chemistry, Saarland University, Campus Building E 8.1, 66123 Saarbr├╝cken, Germany. Electronic address: anna.hirsch@helmholtz-hzi.de.

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.

KEYWORDS:

Anti-inflammatory; Budesonide; Drug delivery; Lipid-DNA; Solubility

PMID:
29908939
DOI:
10.1016/j.ejpb.2018.06.012

Supplemental Content

Full text links

Icon for Elsevier Science
Loading ...
Support Center