Bioavailability of capsaicin and its implications for drug delivery.
Bioavailability of capsaicin and its implications for drug delivery.
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DOI：
10.1016/j.jconrel.2014.09.027
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发表时间：
2014-12-28
期刊：
影响因子：
--
通讯作者：
Dasgupta P
中科院分区：
文献类型：
--
作者：
Rollyson WD;Stover CA;Brown KC;Perry HE;Stevenson CD;McNees CA;Ball JG;Valentovic MA;Dasgupta P
膳食化合物辣椒素是辣椒和辣椒提取物的“辛辣”味道的原因。它是一种有价值的药理学试剂，在控制疼痛和炎症方面具有多种治疗应用。新兴的研究表明，它在几种人类癌症中显示出有效的抗肿瘤活性。在更基础的研究水平上，辣椒素已被用作激活几种类型的离子通道受体的配体。辣椒素样化合物的药理学活性取决于几个因素，如剂量、给药途径，最重要的是取决于其在靶组织的浓度。本文综述了辣椒素类化合物在啮齿类动物和人类中的代谢和生物利用度。本文详细讨论了用于提高辣椒素生物利用度和治疗指数的新型给药策略。新的辣椒素模拟物和改进的药物递送方法的产生将促进辣椒素在人类疾病中的创新应用的希望。
The dietary compound capsaicin is responsible for the “hot and spicy” taste of chili peppers and pepper extracts. It is a valuable pharmacological agent with several therapeutic applications in controlling pain and inflammation. Emerging studies show that it displays potent anti-tumor activity in several human cancers. On a more basic research level, capsaicin has been used as a ligand to activate several types of ion-channel receptors. The pharmacological activity of capsaicin-like compounds is dependent on several factors like the dose, the route of administration and most importantly on its concentration at target tissues. The present review describes the current knowledge involving the metabolism and bioavailability of capsaicinoids in rodents and humans. Novel drug delivery strategies used to improve the bioavailability and therapeutic index of capsaicin are discussed in detail. The generation of novel capsaicin-mimetics and improved drug delivery methods will foster the hope of innovative applications of capsaicin in human disease.
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通过制备包合物提高辣椒素的水溶性和生物利用度
影响因子：
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作者：
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