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纳米颗粒制剂增强具有潜在抗癌特性的疏水性多酚的肿瘤靶向性。

Nanoparticle formulations to enhance tumor targeting of poorly soluble polyphenols with potential anticancer properties.

机构信息

Department of Drug Sciences, University of Pavia, Vle Taramelli 12, 27110 Pavia, Italy.

Department of Drug Sciences, University of Pavia, Vle Taramelli 12, 27110 Pavia, Italy.

出版信息

Semin Cancer Biol. 2017 Oct;46:205-214. doi: 10.1016/j.semcancer.2017.06.010. Epub 2017 Jul 1.

DOI:10.1016/j.semcancer.2017.06.010
PMID:28673607
Abstract

Polyphenols have been extensively studied for their relevant anticancer activity. Quite often however their instability, extensive metabolization, low bioavailability and poor solubility limit their application in cancer prevention and therapy. Formulation in nanoparticles has been widely proposed as a means to overcome these limits, maximize localization and specific activity at tumor site. The present review is intended as an update of literature regarding nanoparticulate carriers aimed to deliver polyphenols to the cancer site. Three molecules were chosen, all of which were hydrophobic and poorly soluble, representative of different polyphenol classes: quercetin (QT) among the flavonoid group, curcumin (CUR) as representative of curcuminoids, and resveratrol (RSV) among the stilbenes. In particular, nanoparticulate systems suitable for poorly soluble drugs will be described and attention will be paid to characteristics designed to improve tumor targeting, specific delivery and interaction with tumor cells.

摘要

多酚因其相关的抗癌活性而被广泛研究。然而,它们的不稳定性、广泛的代谢、低生物利用度和较差的溶解度限制了它们在癌症预防和治疗中的应用。纳米颗粒制剂已被广泛提出作为克服这些限制、最大限度地将药物定位于肿瘤部位并提高其特异性活性的手段。本综述旨在更新有关旨在将多酚递送至肿瘤部位的纳米载体的文献。选择了三种疏水性和低溶解性的分子,它们代表了不同的多酚类:类黄酮组中的槲皮素 (QT)、姜黄素类中的姜黄素 (CUR) 以及二苯乙烯类中的白藜芦醇 (RSV)。特别地,将描述适合难溶性药物的纳米颗粒系统,并将注意力集中在旨在改善肿瘤靶向、特异性递药和与肿瘤细胞相互作用的特性上。

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