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用于治疗肥胖症的藤黄提取物口腔原位凝胶液体制剂的研发

Development of Oral In Situ Gelling Liquid Formulations of Garcinia Extract for Treating Obesity.

作者信息

Fungfoung Kantiya, Praparatana Rachanida, Issarachot Ousanee, Wiwattanapatapee Ruedeekorn

机构信息

Department of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hatyai 90112, Songkhla, Thailand.

Faculty of Medical Technology, Prince of Songkla University, Hatyai 90112, Songkhla, Thailand.

出版信息

Gels. 2023 Aug 16;9(8):660. doi: 10.3390/gels9080660.

Abstract

Novel in situ gelling liquid formulations incorporating garcinia extract were developed to achieve prolonged delivery of hydroxycitric acid (HCA), an active compound displaying anti-obesity function, following oral administration. The optimized formulation was composed of sodium alginate (1.5% /), hydroxypropyl methylcellulose (HPMC K100) (0.25% /), calcium carbonate (1% /) and garcinia extract (2% /). The formulation displayed rapid gelation in less than a minute on exposure to 0.1 N hydrochloric acid (pH 1.2) and remained afloat for more than 24 h. The formulations were capable of gradually releasing more than 80% of HCA load over 8 h, depending on the composition. The resulting gels exhibited high values of gel strength by texture analysis, suggesting they would offer resistance to breakdown under the action of stomach content movement. The optimized formulation loaded garcinia extract significantly reduced lipid accumulation in 3T3-L1 adipocyte cells and displayed moderate anti-inflammatory activity by inhibiting the production of nitric oxide (NO) in LPS-stimulated RAW 264.7 macrophage cells. These findings demonstrate that oral in situ gelling liquid formulations based on sodium alginate and HPMC K100 offer much potential for sustained delivery of HCA and other anti-obesity compounds.

摘要

开发了包含藤黄提取物的新型原位凝胶液体制剂,以实现口服给药后具有抗肥胖功能的活性化合物羟基柠檬酸(HCA)的长效递送。优化后的制剂由海藻酸钠(1.5% /)、羟丙基甲基纤维素(HPMC K100)(0.25% /)、碳酸钙(1% /)和藤黄提取物(2% /)组成。该制剂在暴露于0.1 N盐酸(pH 1.2)时不到一分钟即可快速凝胶化,并能漂浮超过24小时。根据组成不同,这些制剂能够在8小时内逐渐释放超过80%的HCA负载量。通过质地分析,所得凝胶表现出较高的凝胶强度值,表明它们在胃内容物运动的作用下能够抵抗分解。负载藤黄提取物的优化制剂显著减少了3T3-L1脂肪细胞中的脂质积累,并通过抑制脂多糖刺激的RAW 26,4.7巨噬细胞中一氧化氮(NO)的产生而表现出适度的抗炎活性。这些发现表明,基于海藻酸钠和HPMC K100的口服原位凝胶液体制剂在HCA和其他抗肥胖化合物的持续递送方面具有很大潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ddc2/10453886/34126468df7a/gels-09-00660-g001.jpg

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