Enhanced bioavailability and bioefficacy of an amorphous solid dispersion of curcumin

被引:91
作者
Chuah, Ai Mey [1 ]
Jacob, Bindya [1 ]
Jie, Zhang [1 ]
Ramesh, Subbarayan [3 ]
Mandal, Shibajee [3 ]
Puthan, Jithesh K. [3 ]
Deshpande, Parag [3 ]
Vaidyanathan, Vadakkanchery V. [3 ]
Gelling, Richard W. [1 ]
Patel, Gaurav [2 ]
Das, Tapas [2 ]
Shreeram, Sathyavageeswaran [1 ]
机构
[1] Abbott Nutr Res & Dev, Singapore 138668, Singapore
[2] Abbott Nutr Res & Dev, Columbus, OH 43219 USA
[3] Syngene Int Ltd, Bangalore 560099, Karnataka, India
关键词
Curcumin; Melt-extrusion; Amorphous; solid dispersion; Bioavailability; Bio-efficacy; INDUCED PULMONARY-FIBROSIS; ORAL BIOAVAILABILITY; ENCAPSULATED CURCUMIN; IN-VITRO; PROLIFERATION; INHIBITION; ABSORPTION; APOPTOSIS; COMPLEX; CELLS;
D O I
10.1016/j.foodchem.2014.01.108
中图分类号
O69 [应用化学];
学科分类号
081704 ;
摘要
Curcumin has been shown to have a wide variety of biological activities for various human diseases including inflammation, diabetes and cancer. However, the poor oral bioavailability of curcumin poses a significant pharmacological barrier to its use therapeutically and/or as a functional food. Here we report the evaluation of the bioavailability and bio-efficacy of curcumin as an amorphous solid dispersion (ASD) in a matrix consisting of hydroxypropyl methyl cellulose (HPMC), lecithin and isomalt using hot melt extrusion for application in food products. Oral pharmacokinetic studies in rats showed that ASD curcumin was similar to 13-fold more bioavailable compared to unformulated curcumin. Evaluation of the anti-inflammatory activity of ASD curcumin in vivo demonstrated enhanced bio-efficacy compared to unformulated curcumin at 10-fold lower dose. Thus ASD curcumin provides a more potent and efficacious formulation of curcumin which may also help in masking the colour, taste and smell which currently limit its application as a functional food ingredient. (C) 2014 Elsevier Ltd. All rights reserved.
引用
收藏
页码:227 / 233
页数:7
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