Affordable Access

Access to the full text

A Lipid Micellar System Loaded with Dexamethasone Palmitate Alleviates Rheumatoid Arthritis

Authors
  • Wang, Xinxin
  • Feng, Yan
  • Fu, Jijun
  • Wu, Cuishuan
  • He, Bing
  • Zhang, Hua
  • Wang, Xueqing
  • Dai, Wenbing
  • Sun, Yong
  • Zhang, Qiang
Type
Published Article
Journal
AAPS PharmSciTech
Publisher
American Association of Pharmaceutical Scientists
Publication Date
Oct 10, 2019
Volume
20
Issue
8
Identifiers
DOI: 10.1208/s12249-019-1449-1
Source
Springer Nature
Keywords
License
Yellow

Abstract

Glucocorticoids have been confirmed to be effective in the treatment of a variety of inflammatory diseases. However, their application encounters limitations in terms of tissue distribution and bioavailability in vivo. To address these key issues, we designed and developed a nanopreparation by using egg yolk lecithin/sodium glycocholate (EYL/SGC) and utilize such mixed micelles (MMs) to encapsulate dexamethasone palmitate (DMP) for the treatment of rheumatoid arthritis (RA). The prepared DMP-MMs had an average particle size of 49.18 ± 0.43 nm and were compared with an emulsion-based dexamethasone palmitate. Pharmacokinetic and in vivo fluorescence imaging showed that mixed micelles had higher bioavailability and targeting efficiency in inflammatory sites. An arthritis rat model was established via induction by Complete Freund’s Adjuvant (CFA), followed by the efficacy studies by the observations of paw volume, histology, spleen index, pro-inflammatory cytokines, and CT images. It was confirmed that intravenous injection of DMP-MMs exhibited advantages in alleviating joint inflammation compared with the emulsion system. Composed of pharmaceutical adjuvants only, the nanoscale mixed micelles seem a promising carrier system for the RA treatment with lipophilic drugs.

Report this publication

Statistics

Seen <100 times