title: Enhanced bioavailability and bioefficacy of an amorphous solid dispersion of curcumin.
abstract: 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 ∼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.
authors.affiliation: Abbott Nutrition Research and Development, 20 Biopolis Way, Singapore 138668, Singapore.
authors.forename: Ai Mey
authors.initials: AM
authors.lastname: Chuah
authors.affiliation: Abbott Nutrition Research and Development, 20 Biopolis Way, Singapore 138668, Singapore.
authors.forename: Bindya
authors.initials: B
authors.lastname: Jacob
authors.affiliation: Abbott Nutrition Research and Development, 20 Biopolis Way, Singapore 138668, Singapore.
authors.forename: Zhang
authors.initials: Z
authors.lastname: Jie
authors.affiliation: Syngene International Limited, Biocon Park, Plot 2 & 3 Bommasandra 4th Phase, Jigani Link Road, Bangalore 560099, India.
authors.forename: Subbarayan
authors.initials: S
authors.lastname: Ramesh
authors.affiliation: Syngene International Limited, Biocon Park, Plot 2 & 3 Bommasandra 4th Phase, Jigani Link Road, Bangalore 560099, India.
authors.forename: Shibajee
authors.initials: S
authors.lastname: Mandal
authors.affiliation: Syngene International Limited, Biocon Park, Plot 2 & 3 Bommasandra 4th Phase, Jigani Link Road, Bangalore 560099, India.
authors.forename: Jithesh K
authors.initials: JK
authors.lastname: Puthan
authors.affiliation: Syngene International Limited, Biocon Park, Plot 2 & 3 Bommasandra 4th Phase, Jigani Link Road, Bangalore 560099, India.
authors.forename: Parag
authors.initials: P
authors.lastname: Deshpande
authors.affiliation: Syngene International Limited, Biocon Park, Plot 2 & 3 Bommasandra 4th Phase, Jigani Link Road, Bangalore 560099, India.
authors.forename: Vadakkanchery V
authors.initials: VV
authors.lastname: Vaidyanathan
authors.affiliation: Abbott Nutrition Research and Development, 20 Biopolis Way, Singapore 138668, Singapore.
authors.forename: Richard W
authors.initials: RW
authors.lastname: Gelling
authors.affiliation: Abbott Nutrition Research and Development, 3300 Stelzer Road, Columbus, OH 43219, USA.
authors.forename: Gaurav
authors.initials: G
authors.lastname: Patel
authors.affiliation: Abbott Nutrition Research and Development, 3300 Stelzer Road, Columbus, OH 43219, USA.
authors.forename: Tapas
authors.initials: T
authors.lastname: Das
authors.affiliation: Abbott Nutrition Research and Development, 20 Biopolis Way, Singapore 138668, Singapore. Electronic address: shreeram.sathya@abbott.com.
authors.forename: Sathyavageeswaran
authors.initials: S
authors.lastname: Shreeram
mesh_terms: D000818:Animals; D001682:Biological Availability; D003474:Curcumin / Q000493:pharmacokinetics / Q000494:pharmacology*; D006801:Humans; D051381:Rats
chemical_list: D003474:Curcumin
keywords: Amorphous solid dispersion; Bio-efficacy; Bioavailability; Curcumin; Melt-extrusion