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载槲皮素纳米乳凝胶治疗类风湿关节炎的体内外研究。

Quercetin loaded nanoemulsion-based gel for rheumatoid arthritis: In vivo and in vitro studies.

机构信息

Department of Pharmaceutics, R.C. Patel Institute of Pharmaceutical Education and Research, Shirpur, Maharashtra, India.

Department of Pharmaceutics, R.C. Patel Institute of Pharmaceutical Education and Research, Shirpur, Maharashtra, India.

出版信息

Biomed Pharmacother. 2019 Apr;112:108622. doi: 10.1016/j.biopha.2019.108622. Epub 2019 Feb 21.

DOI:10.1016/j.biopha.2019.108622
PMID:30797146
Abstract

Current research reports the development, optimization and evaluation of Quercetin (QCT) loaded nanoemulsion (NE)-based gel for the effective rheumatoid arthritis (RA) management. The formulation of QCT- NE was developed using spontaneous emulsification techniques using the Box- Behnken experimental design. The cytotoxicity study and effect on TNF-α production were evaluated respectively on HIG-82 and RAW 264.7 cells. The study showed that QCT- NE has no toxic effect on synoviocytes and a strong inhibitory effect on LPS-induced TNF-α production. QCT- NE gel has confirmed adequate rheological behavior with a good texture profile and improved drug permeation compared to free QCT gel. In addition, the gel was found to be non-irritating and showed the inhibition of paw edema in rats induced by CFA over 24 h contrary to free QCT gel. In conclusion, the formulation of QCT- NE gel is an efficient topical treatment strategy for rheumatoid arthritis.

摘要

目前的研究报告了载有槲皮素(QCT)的纳米乳(NE)的开发、优化和评估,该制剂用于有效的类风湿关节炎(RA)管理。使用 Box-Behnken 实验设计的自发乳化技术开发了 QCT-NE 的配方。分别在 HIG-82 和 RAW 264.7 细胞上评估了细胞毒性研究和对 TNF-α 产生的影响。研究表明,QCT-NE 对滑膜细胞没有毒性作用,并且对 LPS 诱导的 TNF-α 产生有很强的抑制作用。与游离 QCT 凝胶相比,QCT-NE 凝胶具有足够的流变行为,良好的质地特征,并且改善了药物渗透。此外,与游离 QCT 凝胶相比,该凝胶被发现对 CFA 诱导的大鼠爪肿胀没有刺激性,并且在 24 小时内抑制了爪肿胀。总之,QCT-NE 凝胶的配方是治疗类风湿关节炎的有效局部治疗策略。

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