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目的:α-倒捻子素（α-mangostin,MG）是一种具有潜在的抗风湿活性的多酚。为改善其药动学特性，我们制备了MG的微乳体系（MG-loaded microemulsion,MG-ME），本研究拟进一步揭示MG-ME可能存在的增效性特征。方法: 本研究分析比较了MG-ME相对于其溶液在细胞摄取率、增殖抑制率、通路调控能力及体内关节保护效率等方面的差异。体外实验采用类风湿关节炎成纤维样滑膜细胞（HFLS-RA）为研究对象，MG在细胞内分布采用HPLC法测定，细胞活力采用MTT法测定，通路的调控作用采用Western blot法检测，体内药效以对佐剂性关节炎（adjuvant-induced arthritis,AA）大鼠的治疗效果为依据。结果: 微乳显著提高了细胞对于MG的摄取，强化了MG对HFLS-RA细胞中p38和NF-κB信号通路的调控，并对该细胞的体外增殖产生更为高效的抑制作用；同时相对于溶液体系，MG-ME进一步改善了药物对AA大鼠的关节保护作用。结论:结果表明微乳能增强滑膜组织对于MG的摄取，提高滑膜细胞对于药物刺激的敏感性，从而切实提高药物的体内疗效，是极具潜力且值得深入研究的抗风湿药物的有效载体。
OBJECTIVE: Alpha-mangostin (MG) is a polyphenol with potential antirheumatic activity. To improve the pharmacokinetics of MG, we prepared MG-loaded microemulsion (MG-ME). This study is to further reveal the potential synergistic characteristics of MG-ME. Methods: This study analyzed and compared the MG-ME relative to its solution in the cell uptake rate, inhibition rate of proliferation, pathway regulation and control efficiency and other aspects of the efficiency of joint protection. The rheumatoid arthritis fibroblast-like synoviocytes (HFLS-RA) were used as the research object in vitro. The intracellular distribution of MG was determined by HPLC. The viability of the cells was determined by MTT assay. The function of the pathway was detected by Western blot. The efficacy is based on the therapeutic effect on adjuvant-induced arthritis (AA) rats. RESULTS: Microemulsion significantly increased cellular uptake of MG, enhanced MG regulation of p38 and NF-κB signaling in HFLS-RA cells, and produced more efficient inhibition of proliferation in vitro. Meanwhile, Solution system, MG-ME to further improve the joint protective effect of drugs on AA rats. Conclusion: The results show that microemulsion can enhance the uptake of MG in synovial tissue and increase the sensitivity of synovial cells to drug stimulation, so as to effectively improve the in vivo therapeutic effect of the drug, which is an effective vector worthy of further study on antirheumatic drugs .