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用于肥胖治疗中羟基柠檬酸控释的高膨胀天然复合膜

High-Expansion Natural Composite Films for Controlled Delivery of Hydroxycitric Acid in Obesity Therapy.

作者信息

Fungfoung Kantiya, Issarachot Ousanee, Praparatana Rachanida, Wiwattanapatapee Ruedeekorn

机构信息

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

Department of Pharmacy Technician, Faculty of Public Health and Allied Health Sciences, Sirindhorn College of Public Health Trang, Praboromrajchanok Institute, 89 M.2 Kantang District, Trang 92110, Thailand.

出版信息

Polymers (Basel). 2025 Jun 18;17(12):1697. doi: 10.3390/polym17121697.

DOI:10.3390/polym17121697
PMID:40574227
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12196857/
Abstract

Expandable films represent a promising gastroretentive drug delivery system, offering prolonged gastric retention and sustained drug release features particularly advantageous for obesity treatment. This study developed high-expansion films using konjac and various low glycemic index starches, including purple potato, brown rice, resistant, and red jasmine rice starches, in combination with chitosan and hydroxypropyl methylcellulose (HPMC) E15. Garcinia extract was incorporated into the films using the solvent casting technique. Among 27 formulations, all demonstrated rapid unfolding (within 15 min) and significant expansion (2-4 folds). Hydroxycitric acid (HCA), the active component, was encapsulated at efficiencies exceeding 80% /. The konjac-based films exhibited favorable mechanical properties, expansion capacity, and drug content uniformity. Notably, the CK3-H1 formulation (2% / chitosan, 3% / konjac, 1% / HPMC E15) provided sustained HCA release over 8 h via diffusion. Cytotoxicity tests showed no toxic effects on RAW 264.7 macrophages at concentrations up to 400 μg/mL. Furthermore, CK3-H1 achieved notable nitric oxide inhibition (35.80 ± 1.21%) and the highest reduction in lipid accumulation (31.09 ± 3.15%) in 3T3-L1 adipocytes, outperforming pure HCA and garcinia extract. These results suggest that expandable konjac-based films are a viable and effective delivery system for herbal anti-obesity agents.

摘要

可膨胀薄膜是一种很有前景的胃滞留药物递送系统,具有延长胃滞留时间和持续释药的特性,对肥胖治疗特别有利。本研究利用魔芋与各种低血糖指数淀粉(包括紫薯、糙米、抗性淀粉和红茉莉米淀粉),结合壳聚糖和羟丙基甲基纤维素(HPMC)E15,开发了高膨胀薄膜。采用溶剂浇铸技术将藤黄提取物掺入薄膜中。在27种配方中,所有配方均表现出快速展开(15分钟内)和显著膨胀(2至4倍)。活性成分羟基柠檬酸(HCA)的包封效率超过80%。魔芋基薄膜表现出良好的机械性能、膨胀能力和药物含量均匀性。值得注意的是,CK3-H1配方(2%壳聚糖、3%魔芋、1%HPMC E15)通过扩散在8小时内实现了HCA的持续释放。细胞毒性试验表明,在浓度高达400μg/mL时,对RAW 264.7巨噬细胞无毒性作用。此外,CK3-H1在3T3-L1脂肪细胞中实现了显著的一氧化氮抑制(35.80±1.21%)和脂质积累的最大减少(31.09±3.15%),优于纯HCA和藤黄提取物。这些结果表明,基于魔芋的可膨胀薄膜是一种可行且有效的草药抗肥胖剂递送系统。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a6f2/12196857/9099b0a37b85/polymers-17-01697-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a6f2/12196857/b0d5b5de82bb/polymers-17-01697-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a6f2/12196857/7ade60b78e5f/polymers-17-01697-g002a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a6f2/12196857/bd7e63d264f0/polymers-17-01697-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a6f2/12196857/8bd40969a0dc/polymers-17-01697-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a6f2/12196857/3abd907a7eda/polymers-17-01697-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a6f2/12196857/a0904a565134/polymers-17-01697-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a6f2/12196857/2c23caf6b8cb/polymers-17-01697-g007a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a6f2/12196857/da04a23464d1/polymers-17-01697-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a6f2/12196857/9099b0a37b85/polymers-17-01697-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a6f2/12196857/b0d5b5de82bb/polymers-17-01697-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a6f2/12196857/7ade60b78e5f/polymers-17-01697-g002a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a6f2/12196857/bd7e63d264f0/polymers-17-01697-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a6f2/12196857/8bd40969a0dc/polymers-17-01697-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a6f2/12196857/3abd907a7eda/polymers-17-01697-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a6f2/12196857/a0904a565134/polymers-17-01697-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a6f2/12196857/2c23caf6b8cb/polymers-17-01697-g007a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a6f2/12196857/da04a23464d1/polymers-17-01697-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a6f2/12196857/9099b0a37b85/polymers-17-01697-g009.jpg

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