Delivery system for budesonide based on lipid-DNA

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.

<p>Synthesis of budesonide conjugates and their anti-inflammatory effects: a preliminary study</p>

“…Compared with other glucocorticoids in this class, Bud has stronger local anti-inflammatory and pharmaceutical effects, a longer action time, and a less systemic action; therefore, it could significantly reduce the adverse reactions when used in local treatment 6,7. However, the poor water solubility of Bud affects its dissolution and release behavior, thus influencing the drug concentration at the inflammatory site and its local bioavailability 8,9…”

Lipid–oligonucleotide conjugates for bioapplications

“…Recently, Liu et al. delivered budesonide (sold as SYMBICORT, a glucocorticoid for treating chronic inflammation) through a UU11mer DNA–lipid micelle system, showing better drug solubility in the water phase and good anti-inflammatory activity [ 82 ]. In another study from Charbgoo et al , doxorubicin (DOX), a widely used hydrophilic chemotherapy medication for treating multiple types of cancer, preferentially intercalated into double-stranded GC-rich regions in cholesteryl-modified MUC1 aptamer micelles, resulting in enhanced specific therapeutic effects with reduced DOX dosage in both in vitro and in vivo studies [ 80 ].…”