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Enhancement of curcumin oral absorption and pharmacokinetics of curcuminoids and curcumin metabolites in mice
by
Chen, Wei
, Fan-Havard, Patty
, Yee, Lisa D.
, Yen, Winston
, Chan, Kenneth K.
, Wang, Jiang
, Chiu, Ming
, Zhongfa, Liu
in
Absorption
/ Administration, Oral
/ Animals
/ Antineoplastic agents
/ Biological and medical sciences
/ Biological Availability
/ Cancer Research
/ Chromatography, High Pressure Liquid
/ Curcumin - analogs & derivatives
/ Curcumin - pharmacokinetics
/ Dose-Response Relationship, Drug
/ Drug Stability
/ Emulsions
/ Medical sciences
/ Medicine
/ Medicine & Public Health
/ Mice
/ Mice, Inbred Strains
/ Microscopy, Electron, Transmission
/ Molecular Structure
/ Mouth Mucosa - metabolism
/ Nanoparticles
/ Oncology
/ Original Article
/ Particle Size
/ Pharmacology. Drug treatments
/ Pharmacology/Toxicology
/ Solubility
/ Surface Properties
/ Tandem Mass Spectrometry
2012
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Enhancement of curcumin oral absorption and pharmacokinetics of curcuminoids and curcumin metabolites in mice
by
Chen, Wei
, Fan-Havard, Patty
, Yee, Lisa D.
, Yen, Winston
, Chan, Kenneth K.
, Wang, Jiang
, Chiu, Ming
, Zhongfa, Liu
in
Absorption
/ Administration, Oral
/ Animals
/ Antineoplastic agents
/ Biological and medical sciences
/ Biological Availability
/ Cancer Research
/ Chromatography, High Pressure Liquid
/ Curcumin - analogs & derivatives
/ Curcumin - pharmacokinetics
/ Dose-Response Relationship, Drug
/ Drug Stability
/ Emulsions
/ Medical sciences
/ Medicine
/ Medicine & Public Health
/ Mice
/ Mice, Inbred Strains
/ Microscopy, Electron, Transmission
/ Molecular Structure
/ Mouth Mucosa - metabolism
/ Nanoparticles
/ Oncology
/ Original Article
/ Particle Size
/ Pharmacology. Drug treatments
/ Pharmacology/Toxicology
/ Solubility
/ Surface Properties
/ Tandem Mass Spectrometry
2012
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Enhancement of curcumin oral absorption and pharmacokinetics of curcuminoids and curcumin metabolites in mice
by
Chen, Wei
, Fan-Havard, Patty
, Yee, Lisa D.
, Yen, Winston
, Chan, Kenneth K.
, Wang, Jiang
, Chiu, Ming
, Zhongfa, Liu
in
Absorption
/ Administration, Oral
/ Animals
/ Antineoplastic agents
/ Biological and medical sciences
/ Biological Availability
/ Cancer Research
/ Chromatography, High Pressure Liquid
/ Curcumin - analogs & derivatives
/ Curcumin - pharmacokinetics
/ Dose-Response Relationship, Drug
/ Drug Stability
/ Emulsions
/ Medical sciences
/ Medicine
/ Medicine & Public Health
/ Mice
/ Mice, Inbred Strains
/ Microscopy, Electron, Transmission
/ Molecular Structure
/ Mouth Mucosa - metabolism
/ Nanoparticles
/ Oncology
/ Original Article
/ Particle Size
/ Pharmacology. Drug treatments
/ Pharmacology/Toxicology
/ Solubility
/ Surface Properties
/ Tandem Mass Spectrometry
2012
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Enhancement of curcumin oral absorption and pharmacokinetics of curcuminoids and curcumin metabolites in mice
Journal Article
Enhancement of curcumin oral absorption and pharmacokinetics of curcuminoids and curcumin metabolites in mice
2012
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Overview
Purpose
Curcumin has shown a variety of biological activity for various human diseases including cancer in preclinical setting. Its poor oral bioavailability poses significant pharmacological barriers to its clinical application. Here, we established a practical nano-emulsion curcumin (NEC) containing up to 20% curcumin (w/w) and conducted the pharmacokinetics of curcuminoids and curcumin metabolites in mice.
Methods
This high loading NEC was formulated based on the high solubility of curcumin in polyethylene glycols (PEGs) and the synergistic enhancement of curcumin absorption by PEGs and Cremophor EL. The pharmacokinetics of curcuminoids and curcumin metabolites was characterized in mice using a LC–MS/MS method, and the pharmacokinetic parameters were determined using WinNonlin computer software.
Results
A tenfold increase in the
AUC
0→24h
and more than 40-fold increase in the
C
max
in mice were observed after an oral dose of NEC compared with suspension curcumin in 1% methylcellulose. The plasma pharmacokinetics of its two natural congeners, demethoxycurcumin and bisdemethoxycurcumin, and three metabolites, tetrahydrocurcumin (THC), curcumin-
O
-glucuronide, and curcumin-
O
-sulfate, was characterized for the first time in mice after an oral dose of NEC.
Conclusion
This oral absorption enhanced NEC may provide a practical formulation to conduct the correlative study of the PK of curcuminoids and their pharmacodynamics, e.g., hypomethylation activity in vivo.
Publisher
Springer-Verlag,Springer,Springer Nature B.V
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