A Critical Appraisal of Solubility Enhancement Techniques of Polyphenols.
A Critical Appraisal of Solubility Enhancement Techniques of Polyphenols.
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DOI：
10.1155/2014/180845
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发表时间：
2014
影响因子：
--
通讯作者：
Kaur G
中科院分区：
文献类型：
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作者：
Kaur H;Kaur G
多酚是植物界广泛分布的一类天然物质。这些是由植物产生的次级代谢产物，迄今为止已经确定了8000个代表。最近，由于多酚在预防退行性疾病如神经退行性疾病、癌症和心血管疾病中的作用的证据，对多酚的兴趣增加。虽然市场上有大量的药物可用于治疗这些疾病，但是，目前的重点是利用来自植物的天然成分。大多数多酚显示出低的体内生物利用度，因此限制了它们用于口服药物递送的应用。这种低生物利用度可能与低水溶性、首过效应、GIT中的代谢或与细胞DNA和蛋白质的不可逆结合有关。因此，需要设计改善多酚的口服生物利用度的策略。纳米化、自微乳化给药系统（SMEDDS）、微囊化、络合和固体分散等多种方法可用于提高生物利用度。本文将重点介绍迄今为止已采用的各种方法，以提高各种多酚的溶解度，从而可以配制合适的药物递送系统。
Polyphenols constitute a family of natural substances distributed widely in plant kingdom. These are produced as secondary metabolites by plants and so far 8000 representatives of this family have been identified. Recently, there is an increased interest in the polyphenols because of the evidence of their role in prevention of degenerative diseases such as neurodegenerative diseases, cancer, and cardiovascular diseases. Although a large number of drugs are available in the market for treatment of these diseases, however, the emphasis these days is on the exploitation of natural principles derived from plants. Most polyphenols show low in vivo bioavailability thus limiting their application for oral drug delivery. This low bioavailability could be associated with low aqueous solubility, first pass effect, metabolism in GIT, or irreversible binding to cellular DNA and proteins. Therefore, there is a need to devise strategies to improve oral bioavailability of polyphenols. Various approaches like nanosizing, self-microemulsifying drug delivery systems (SMEDDS), microencapsulation, complexation, and solid dispersion can be used to increase the bioavailability. This paper will highlight the various methods that have been employed till date for the solubility enhancement of various polyphenols so that a suitable drug delivery system can be formulated.