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新型载咖啡因溶解微针贴片对高脂肪饮食诱导肥胖 C57BL/6J 小鼠的减肥作用。

Anti-obesity effect of a novel caffeine-loaded dissolving microneedle patch in high-fat diet-induced obese C57BL/6J mice.

机构信息

Department of Biotechnology, Building 123, Yonsei University, 50 Yonsei-ro, Seodaemun-gu, Seoul 03722, Republic of Korea.

Department of Biotechnology, Building 123, Yonsei University, 50 Yonsei-ro, Seodaemun-gu, Seoul 03722, Republic of Korea; Juvic Biotech, Inc., Building 102, Yonsei Engineering Research Park, 50 Yonsei-ro, Seodaemun-gu, Seoul 03722, Republic of Korea.

出版信息

J Control Release. 2017 Nov 10;265:41-47. doi: 10.1016/j.jconrel.2017.03.400. Epub 2017 Apr 4.

Abstract

Natural products such as caffeine have been found to be effective in reducing body weight through lipolysis. Here, we report the successful loading of caffeine onto dissolving microneedle following inhibition of its crystal growth by hyaluronic acid (HA), the matrix material of the dissolving microneedle (DMN). Further, the anti-obesity activity of caffeine was evaluated in high-fat diet-induced obese C57BL/6J mice. After 6weeks of caffeine loaded dissolving microneedle patch (CMP) administration, lipolysis improved significantly as shown by leptin and adiponectin activity, which resulted in considerable weight loss of about 12.8±0.75% in high-fat diet-induced obese mice. Comparison of the levels of triglyceride, total cholesterol, high-density lipoprotein (HDL)-cholesterol, and low-density lipoprotein (LDL)-cholesterol after CMP administration with the initial levels in obese mice indicated significant anti-obesity activity of CMP. These findings suggested that a novel CMP with an increased amount of caffeine loaded onto DMN has therapeutic activity against obesity.

摘要

天然产物,如咖啡因,已被发现通过脂肪分解来有效减轻体重。在这里,我们报告了在透明质酸(HA)抑制咖啡因晶体生长的情况下,成功地将咖啡因载入溶解微针中。透明质酸是溶解微针(DMN)的基质材料。此外,还评估了咖啡因在高脂肪饮食诱导的肥胖 C57BL/6J 小鼠中的抗肥胖活性。经过 6 周的咖啡因负载溶解微针贴片(CMP)给药后,脂肪分解显著改善,瘦素和脂联素活性增加,导致高脂肪饮食诱导的肥胖小鼠体重减轻约 12.8±0.75%。与肥胖小鼠初始水平相比,CMP 给药后甘油三酯、总胆固醇、高密度脂蛋白(HDL)-胆固醇和低密度脂蛋白(LDL)-胆固醇水平的比较表明 CMP 具有显著的抗肥胖活性。这些发现表明,一种新型的 CMP 可以将更多的咖啡因载入 DMN,对肥胖症具有治疗作用。

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