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Strategies to improve ellagic acid bioavailability: from natural or semisynthetic derivatives to nanotechnological approaches based on innovative carriers

机译:提高鞣花酸生物利用度的策略:从自然或半合成衍生物到基于创新载体的纳米技术方法

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摘要

Ellagic acid (EA) is a polyphenolic compound whose dietary consumption is mainly associated with the intake of red fruits, including pomegranates, strawberries, blackberries, blackcurrants, raspberries, grapes or dried fruits, like walnuts and almonds. A number of studies indicate that EA exerts health-beneficial effects against several chronic pathologies associated with oxidative damage, including different kinds of cancer, cardiovascular and neurodegenerative diseases. Furthermore, EA possesses wound-healing properties, antibacterial and antiviral effects, and acts as a systemic antioxidant. However, clinical applications of this polyphenol have been hampered and prevented by its poor water solubility (9.7 +/- 3.2 mu g ml(-1)in water) and pharmacokinetic profile (limited absorption rate and plasma half-life <1 h after ingestion of pomegranate juice), properties due to the chemical nature of the organic heterotetracyclic compound. Little has been reported on efficient strategies to enhance EA poor oral bioavailability, including chemical structure modifications, encapsulation within nano-microspheres to be used as carriers, and molecular dispersion in polymer matrices. In this review we summarize the experimental approaches investigated so far in order to improve EA pharmacokinetics, supporting the hypothesis that enhancement in EA solubility is a feasible route for increasing its oral absorption.
机译:鞣花酸(EA)是一种多酚化合物,其膳食消耗主要与红色果实摄入有关,包括石榴,草莓,黑莓,黑醋栗,覆盆子,葡萄或干果,如核桃和杏仁。许多研究表明,EA对与氧化损伤相关的几种慢性病理产生健康有益的效果,包括不同种类的癌症,心血管和神经变性疾病。此外,EA具有伤口愈合性质,抗菌和抗病毒作用,并用作全身抗氧化剂。然而,这种多酚的临床应用已经阻碍并通过其差的水溶性(9.7 +/-3.2μg(-1)在水中)和药代动力学曲线(摄取后有限吸收率和血浆半衰期<1小时石榴汁),由于有机异位谱系化合物的化学性质而导致的性质。据报道,有效的策略,提高EA口腔生物利用度,包括化学结构修饰,纳米微球中的封装用作载体,以及聚合物基质中的分子分散。在本综述中,我们总结了到目前为止调查的实验方法,以改善EA药代动力学,支持EA溶解度增强的假设是增加其口腔吸收的可行途径。

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