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载姜黄素壳聚糖-海藻酸钠复合纳米粒的药代动力学和抗结肠癌特性。

Pharmacokinetic and anti-colon cancer properties of curcumin-containing chitosan-pectinate composite nanoparticles.

机构信息

a The School of Pharmacy, University of Nottingham Malaysia Campus , Semenyih , Selangor , Malaysia.

b School of Pharmacy, University of Nottingham, University Park , Nottingham , UK.

出版信息

J Biomater Sci Polym Ed. 2018 Dec;29(18):2281-2298. doi: 10.1080/09205063.2018.1541500. Epub 2018 Dec 28.

DOI:10.1080/09205063.2018.1541500
PMID:30376409
Abstract

Curcumin, the active ingredient of the rhizome curcuma longa has been extensively studied as an anticancer agent for various types of tumours. However, its efficacy as an anticancer agent is restricted due to poor absorption from the gastrointestinal tract, rapid metabolism and degradation in acidic medium. In the present study, we encapsulated curcumin in chitosan-pectinate nanoparticulate system (CUR-CS-PEC-NPs) for deployment of curcumin to the colon, whereby curcumin is protected against degradative effects in the upper digestive tract, and hence, maintaining its anticancer properties until colon arrival. The CUR-CS-PEC-NPs was taken up by HT-29 colorectal cancer cells which ultimately resulted in a significant reduction in cancer cell propagation. The anti-proliferative effect of the encapsulated curcumin was similar to that of free curcumin at equivalent doses which confirms that the encapsulation process did not impede the anticancer activity of curcumin. The oral bioavailability (C, and AUC) of curcumin in CUR-CS-PEC-NPs was enhanced significantly by 4-folds after 6 hours of treatment compared to free curcumin. Furthermore, the clearance of curcumin from the CUR-CS-PEC-NPs was lower compared to free curcumin. These findings point to the potential application of the CUR-CS-PEC-NPs in the oral delivery of curcumin in the treatment of colon cancer.

摘要

姜黄素是姜黄根茎的活性成分,已被广泛研究作为各种类型肿瘤的抗癌剂。然而,由于其在胃肠道中的吸收不良、在酸性介质中快速代谢和降解,其作为抗癌剂的功效受到限制。在本研究中,我们将姜黄素封装在壳聚糖-果胶纳米颗粒系统(CUR-CS-PEC-NPs)中,以将姜黄素递送到结肠,从而保护姜黄素免受上消化道的降解作用,从而保持其抗癌特性直到到达结肠。CUR-CS-PEC-NPs 被 HT-29 结肠直肠癌细胞摄取,最终导致癌细胞增殖显著减少。包封姜黄素的抗增殖作用与等效剂量的游离姜黄素相似,这证实了封装过程不会阻碍姜黄素的抗癌活性。与游离姜黄素相比,CUR-CS-PEC-NPs 中的姜黄素的口服生物利用度(C 和 AUC)在 6 小时治疗后显著提高了 4 倍。此外,CUR-CS-PEC-NPs 中姜黄素的清除率比游离姜黄素低。这些发现表明 CUR-CS-PEC-NPs 在口服递送至结肠癌治疗中的应用潜力。

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