Microemulsion as the drug delivery system improves inhibitory effects of α-mangostin on synovium

Abstract

Abstract:

AIM: α-Mangostin (MG) is a xanthone with antirheumatic effect. To improve the pharmacokinetic performance, we prepared MG loaded microemulsion (MG-ME). This study was designed to evaluate its potential improvements to therapeutic efficacy. METHODS: Intakes of MG by cells were determined by HPLC. Inhibition on proliferation of cells was assessed by MTT method. Western blot was employed to investigate modulation of MG on transduction pathways. The therapeutic efficacy of MG was evaluated based on the effects on adjuvant induced arthritis in rats. RESULTS: Microemulsion improved the intakes of MG in human fibroblast-like synoviocyte rheumatoid arthritis (HFLS-RA) cells, which resulted in the enhanced inhibition on proliferation of cells and modulations on p38 and NF-κB signalings. Also, this delivery system was found augmenting the protection on joints in vivo. CONCLUSION: Microemulsion improved the intakes of MG and the sensitivity of drug stimulation in HFLS-RA cells. It enhances the dru efficacy in vivo and is a promising delivery system for antirheumatic agents.

Key words: α-Mangostin, HFLS-RA cell, synovium, rheumatoid arthritis, microemulsion

CLC Number:

R965.2

GUO Huixia, TAO Mengqing, ZUO Jian, WANG Weiping. Microemulsion as the drug delivery system improves inhibitory effects of α-mangostin on synovium[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2017, 22(11): 1227-1231.

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