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AAPS PharmSciTech

, 20:316 | Cite as

A Lipid Micellar System Loaded with Dexamethasone Palmitate Alleviates Rheumatoid Arthritis

  • Xinxin Wang
  • Yan Feng
  • Jijun Fu
  • Cuishuan Wu
  • Bing He
  • Hua Zhang
  • Xueqing Wang
  • Wenbing Dai
  • Yong Sun
  • Qiang ZhangEmail author
Research Article

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.

KEY WORDS

mixed micelles nanomedicine passive targeting dexamethasone palmitate rheumatoid arthritis 

Notes

Acknowledgments

We thank Beijing Delivery Pharmaceutical Technology Co., Ltd. for supporting Limethason® and NaOH. We would like to thank members of our laboratory for their help and support.

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Copyright information

© American Association of Pharmaceutical Scientists 2019

Authors and Affiliations

  • Xinxin Wang
    • 1
  • Yan Feng
    • 2
  • Jijun Fu
    • 3
  • Cuishuan Wu
    • 4
  • Bing He
    • 2
  • Hua Zhang
    • 2
  • Xueqing Wang
    • 2
  • Wenbing Dai
    • 2
  • Yong Sun
    • 1
  • Qiang Zhang
    • 2
    Email author
  1. 1.Department of Pharmaceutics, School of PharmacyQingdao UniversityQingdaoChina
  2. 2.Beijing Key Laboratory of Molecular Pharmaceutics and New Drug Delivery Systems, School of Pharmaceutical SciencesPeking UniversityBeijingChina
  3. 3.School of Pharmaceutical ScienceGuangzhou Medical UniversityGuangzhouChina
  4. 4.Beijing Delivery Pharmaceutical Technology Co., LtdBeijingChina

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