Delivery system for budesonide based on lipid-DNA

被引：8

作者：

Liu, Yun ^{[1
,2
]}

Bos, I. Sophie T. ^{[3
]}

Oenema, Tjitske A. ^{[3
]}

Meurs, Herman ^{[3
]}

Maarsingh, Harm ^{[4
]}

Hirsch, Anna K. H. ^{[2
,5
,6
]}

机构：

[1] Guangdong Med Univ, Sch Pharm, Dongguan 523808, Peoples R China

[2] Univ Groningen, Stratingh Inst Chem, Nijenborgh 7, NL-9747 AG Groningen, Netherlands

[3] Univ Groningen, Dept Mol Pharmacol, Antonius Deusinglaan 1, NL-9713 AV Groningen, Netherlands

[4] Palm Beach Atlantic Univ, Lloyd L Gregory Sch Pharm, Dept Pharmaceut Sci, W Palm Beach, FL USA

[5] Helmholtz Ctr Infect Res HZI, Helmholtz Inst Pharmaceut Res Saarland HIPS, Dept Drug Design & Optimizat, Campus Bldg E 8-1, D-66123 Saarbrucken, Germany

[6] Saarland Univ, Med Chem, Dept Pharm, Campus Bldg E 8-1, D-66123 Saarbrucken, Germany

来源：

EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS | 2018年 / 130卷

关键词：

Drug delivery; Anti-inflammatory; Budesonide; Lipid-DNA; Solubility; DRUG-DELIVERY; POLYMERIC MICELLES; THERAPY; PHARMACOKINETICS; CORTICOSTEROIDS; INFLAMMATION; RELEASE; DESIGN; MODEL;

D O I：

10.1016/j.ejpb.2018.06.012

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

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.

引用

页码：123 / 127

页数：5

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