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评价局部药物制剂中辣椒素的体外释放和抗菌性能。

Evaluation of In Vitro Capsaicin Release and Antimicrobial Properties of Topical Pharmaceutical Formulation.

机构信息

Pharmacotherapeutic Research Center, Faculty of Medical Sciences, Aldent University, 1001 Tirana, Albania.

Department of Pharmacy, Faculty of Medicine, University of Medicine, 1001 Tirana, Albania.

出版信息

Biomolecules. 2021 Mar 15;11(3):432. doi: 10.3390/biom11030432.

DOI:10.3390/biom11030432
PMID:33804191
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8001808/
Abstract

(1) Background: Capsaicin is the main capsaicinoid of the genus and it is responsible for the pungent taste. Medical uses of the fruits of chili peppers date from the ancient time until nowadays. Most of all, they are used topically as analgesic in anti-inflammatory diseases as rheumatism, arthritis and in diabetic neuropathy. Reports state that the genus, among other plant genera, is a good source of antimicrobial and antifungal compounds. The aim of this study was the preparation of a pharmaceutical Carbopol-based formulation containing capsaicin and the evaluation of its in vitro release and antimicrobial and antifungal properties. (2) Methods: It was first stabilized with an extraction method from the annuum fruits with 98% ethanol and then the identification and determination of Capsaicin in this extract was realized by HPLC. (3) Results and Conclusions: Rheological analyses revealed that the selected formulation exhibited a pseudo-plastic behavior. In vitro release studies of capsaicin from a Carbopol-based formulation reported that approximately 50% of capsaicin was release within 52 h. Additionally, the Carbopol-based formulation significantly increased the antimicrobial effects of capsaicin towards all tested bacteria and fungi strains.

摘要

(1) 背景:辣椒素是属中的主要辣椒素,它负责辣味。辣椒的药用用途可以追溯到古代,直到现在。最重要的是,它们被用作局部镇痛药,用于治疗炎症性疾病,如风湿病、关节炎和糖尿病性神经病。有报道称,属与其他植物属一样,是抗菌和抗真菌化合物的良好来源。本研究的目的是制备一种含有辣椒素的卡波姆为基础的药物制剂,并评价其体外释放和抗菌、抗真菌性能。(2) 方法:首先采用 98%乙醇从 annuum 果实中提取方法进行稳定化,然后通过 HPLC 对提取物中的辣椒素进行鉴定和定量。(3) 结果与结论:流变学分析表明,所选配方表现出假塑性行为。卡波姆为基础的制剂中辣椒素的体外释放研究表明,大约 50%的辣椒素在 52 小时内释放。此外,卡波姆为基础的制剂显著增强了辣椒素对所有测试的细菌和真菌菌株的抗菌作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9ce2/8001808/683fe378726d/biomolecules-11-00432-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9ce2/8001808/65b1dfbef74c/biomolecules-11-00432-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9ce2/8001808/fef1cd2bf2d9/biomolecules-11-00432-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9ce2/8001808/855ebafecb80/biomolecules-11-00432-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9ce2/8001808/233619f3d7f3/biomolecules-11-00432-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9ce2/8001808/2ec8323e1f48/biomolecules-11-00432-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9ce2/8001808/683fe378726d/biomolecules-11-00432-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9ce2/8001808/65b1dfbef74c/biomolecules-11-00432-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9ce2/8001808/fef1cd2bf2d9/biomolecules-11-00432-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9ce2/8001808/855ebafecb80/biomolecules-11-00432-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9ce2/8001808/233619f3d7f3/biomolecules-11-00432-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9ce2/8001808/2ec8323e1f48/biomolecules-11-00432-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9ce2/8001808/683fe378726d/biomolecules-11-00432-g006.jpg

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