制备新型黄芩苷微乳液透皮给药凝胶并测试其抗痛风效果

IF 3 3区 医学 Q2 PHARMACOLOGY & PHARMACY
Yingzhou Wang , Mingxue Liu , Junjie Li , Peipei Jiang , Di Han , Hongling Zhang , Lingyun Xu , Yinsheng Qiu
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引用次数: 0

摘要

我们曾证实黄芩苷口服对痛风性关节炎(GA)有疗效。本文制备了一种新型的黄芩苷微乳液凝胶(B-MEG),并对其透皮给药治疗痛风性关节炎的效果进行了评估。采用中心复合设计、弗朗兹扩散细胞实验和分割-分裂图设计对 B-MEG 的制备方法和透皮能力进行了筛选和优化。在豚鼠身上进行了皮肤刺激试验。用小鼠进行了抗痛风效果评估。优化的 B-MEG 由 50 % pH 7.4 磷酸盐缓冲盐水、4.48 % 油酸乙酯、31.64 % 吐温 80、13.88 % 甘油、2 % 龙脑、0.5 % 丁香油和 0.5 % 黄原胶组成,黄芩苷含量为 (10.42 ± 0.08) mg/g,粒径为 (15.71 ± 0.41) nm。12 小时后,从 B-MEG 中渗透的黄芩苷累积量为 (672.14 ± 44.11) μg-cm-2。使用 B-MEG 后未观察到明显的皮肤刺激症状。与模型组相比,B-MEG 组明显降低了小鼠的耳廓肿胀率(P < 0.01)和捻发音数量(P < 0.01);还降低了 GA 小鼠模型的爪肿胀率(P < 0.01)和炎症细胞浸润。总之,B-MEG 是一种很有前景的黄芩苷透皮载体,可用作治疗 GA 的潜在疗法。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Preparing a novel baicalin-loaded microemulsion-based gel for transdermal delivery and testing its anti-gout effect

We previously demonstrated that baicalin had efficacy against gouty arthritis (GA) by oral administration. In this paper, a novel baicalin-loaded microemulsion-based gel (B-MEG) was prepared and assessed for the transdermal delivery of baicalin against GA. The preparation method and transdermal capability of B-MEG was screened and optimized using the central composite design, Franz diffusion cell experiments, and the split-split plot design. Skin irritation tests were performed in guinea pigs. The anti-gout effects were evaluated using mice. The optimized B-MEG comprised of 50 % pH 7.4 phosphate buffered saline, 4.48 % ethyl oleate, 31.64 % tween 80, 13.88 % glycerin, 2 % borneol, 0.5 % clove oil and 0.5 % xanthan gum, with a baicalin content of (10.42 ± 0.08) mg/g and particle size of (15.71 ± 0.41) nm. After 12 h, the cumulative amount of baicalin permeated from B-MEG was (672.14 ± 44.11) μg·cm−2. No significant skin irritation was observed following B-MEG application. Compared to the model group, B-MEG groups significantly decreased the rate of auricular swelling (P < 0.01) and number of twists observed in mice (P < 0.01); and also reduced the rate of paw swelling (P < 0.01) and inflammatory cell infiltration in a mouse model of GA. In conclusion, B-MEG represents a promising transdermal carrier for baicalin delivery and can be used as a potential therapy for GA.

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来源期刊
Saudi Pharmaceutical Journal
Saudi Pharmaceutical Journal PHARMACOLOGY & PHARMACY-
CiteScore
6.10
自引率
2.40%
发文量
194
审稿时长
67 days
期刊介绍: The Saudi Pharmaceutical Journal (SPJ) is the official journal of the Saudi Pharmaceutical Society (SPS) publishing high quality clinically oriented submissions which encompass the various disciplines of pharmaceutical sciences and related subjects. SPJ publishes 8 issues per year by the Saudi Pharmaceutical Society, with the cooperation of the College of Pharmacy, King Saud University.
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