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姜黄素与甲基丙烯酸共聚物微囊化后口服生物利用度的提高。

Improvement of Oral Bioavailability of Curcumin upon Microencapsulation with Methacrylic Copolymers.

作者信息

Paolino Donatella, Vero Ada, Cosco Donato, Pecora Tiziana M G, Cianciolo Simona, Fresta Massimo, Pignatello Rosario

机构信息

Department of Experimental and Clinical Medicine, University of Catanzaro "Magna Græcia"Catanzaro, Italy; Interregional Research Center for Food Safety and Health, University of Catanzaro "Magna Græcia"Catanzaro, Italy.

Department of Health Sciences, University of Catanzaro "Magna Græcia" Catanzaro, Italy.

出版信息

Front Pharmacol. 2016 Dec 21;7:485. doi: 10.3389/fphar.2016.00485. eCollection 2016.

Abstract

Curcumin (diferuloymethane; CUR) is a yellow pigment used in traditional medicine throughout history for its anti-inflammatory activity. In the last years, the scientific research has demonstrated that CUR effects are related to the modulation of crucial molecular targets, related to several pathologies including cancer, arthritis, diabetes, Crohn's disease. In this paper, two formulations of microencapsulated CUR obtained by coevaporation with polymethacrylate polymers (Eudragit Retard) were investigated , and , and results were compared by laser confocal microscopy analysis. The permeation of microencapsulated CUR through CaCo-2 monolayers was evaluated . The mucoadhesion and bioadhesion of the CUR-loaded microparticles were evaluated , using E12 and CaCo-2 human intestinal cells, and , by means of excised rat intestinal mucosa. After oral administration to rats, microencapsulated CUR showed a sevenfold increase of bioavailability in respect to the neat drug, with a concomitant reduction of the and a five-fold plasma concentration peak increase.

摘要

姜黄素(二阿魏酰甲烷;CUR)是一种黄色色素,在历史上的传统医学中因其抗炎活性而被使用。在过去几年中,科学研究表明,CUR的作用与关键分子靶点的调节有关,这些靶点与包括癌症、关节炎、糖尿病、克罗恩病在内的多种病理状况相关。在本文中,研究了通过与聚甲基丙烯酸酯聚合物(Eudragit缓释剂)共蒸发获得的两种微囊化CUR制剂,并通过激光共聚焦显微镜分析比较了结果。评估了微囊化CUR透过CaCo-2单层细胞的渗透情况。使用E12和CaCo-2人肠道细胞,并通过切除的大鼠肠黏膜评估了负载CUR的微粒的黏膜黏附性和生物黏附性。给大鼠口服后,微囊化CUR相对于纯药物的生物利用度提高了7倍,同时减少了 ,血浆浓度峰值增加了5倍。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d2f7/5174134/0d43e797ca06/fphar-07-00485-g001.jpg

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