Bioavailability of a Lipidic Formulation of Curcumin in Healthy Human Volunteers

Numerous publications have reported the significant pharmacodynamic activity of Curcumin (CRM) despite low or undetectable levels in plasma. The objective of the present study was to perform a detailed pharmacokinetic evaluation of CRM after the oral administration of a highly bioavailable lipidic f...

Full description

Bibliographic Details
Main Authors: Arvind K. Bansal, Gunjan Kohli, Jyoti K. Paliwal, Manoj Karwa, Bhushan Munjal, Saurabh Arora, Yogesh B. Pawar
Format: Article
Language:English
Published: MDPI AG 2012-10-01
Series:Pharmaceutics
Subjects:
Online Access:http://www.mdpi.com/1999-4923/4/4/517
_version_ 1828150418217107456
author Arvind K. Bansal
Gunjan Kohli
Jyoti K. Paliwal
Manoj Karwa
Bhushan Munjal
Saurabh Arora
Yogesh B. Pawar
author_facet Arvind K. Bansal
Gunjan Kohli
Jyoti K. Paliwal
Manoj Karwa
Bhushan Munjal
Saurabh Arora
Yogesh B. Pawar
author_sort Arvind K. Bansal
collection DOAJ
description Numerous publications have reported the significant pharmacodynamic activity of Curcumin (CRM) despite low or undetectable levels in plasma. The objective of the present study was to perform a detailed pharmacokinetic evaluation of CRM after the oral administration of a highly bioavailable lipidic formulation of CRM (CRM-LF) in human subjects. Cmax, Tmax and AUC0–¥ were found to be 183.35 ± 37.54 ng/mL, 0.60 ± 0.05 h and 321.12 ± 25.55 ng/mL respectively, at a dose of 750 mg. The plasma profile clearly showed three distinct phases, viz., absorption, distribution and elimination. A close evaluation of the primary pharmacokinetic parameters provided valuable insight into the behavior of the CRM after absorption by CRM-LF. CRM-LF showed a lag time (Tlag) of 0.18 h (around 12 min). Pharmacokinetic modeling revealed that CRM-LF followed a two-compartment model with first order absorption, lag time and first order elimination. A high absorption rate constant (K01, 4.51/h) signifies that CRM-LF ensured rapid absorption of the CRM into the central compartment. This was followed by the distribution of CRM from the central to peripheral compartment (K12, 2.69/h). The rate of CRM transfer from the peripheral to central compartment (K21, 0.15/h) was slow. This encourages higher tissue levels of CRM as compared with plasma levels. The study provides an explanation of the therapeutic efficacy of CRM, despite very low/undetectable levels in the plasma.
first_indexed 2024-04-11T21:44:13Z
format Article
id doaj.art-b8d1a91b544f4389904a73b190e928ff
institution Directory Open Access Journal
issn 1999-4923
language English
last_indexed 2024-04-11T21:44:13Z
publishDate 2012-10-01
publisher MDPI AG
record_format Article
series Pharmaceutics
spelling doaj.art-b8d1a91b544f4389904a73b190e928ff2022-12-22T04:01:28ZengMDPI AGPharmaceutics1999-49232012-10-014451753010.3390/pharmaceutics4040517Bioavailability of a Lipidic Formulation of Curcumin in Healthy Human VolunteersArvind K. BansalGunjan KohliJyoti K. PaliwalManoj KarwaBhushan MunjalSaurabh AroraYogesh B. PawarNumerous publications have reported the significant pharmacodynamic activity of Curcumin (CRM) despite low or undetectable levels in plasma. The objective of the present study was to perform a detailed pharmacokinetic evaluation of CRM after the oral administration of a highly bioavailable lipidic formulation of CRM (CRM-LF) in human subjects. Cmax, Tmax and AUC0–¥ were found to be 183.35 ± 37.54 ng/mL, 0.60 ± 0.05 h and 321.12 ± 25.55 ng/mL respectively, at a dose of 750 mg. The plasma profile clearly showed three distinct phases, viz., absorption, distribution and elimination. A close evaluation of the primary pharmacokinetic parameters provided valuable insight into the behavior of the CRM after absorption by CRM-LF. CRM-LF showed a lag time (Tlag) of 0.18 h (around 12 min). Pharmacokinetic modeling revealed that CRM-LF followed a two-compartment model with first order absorption, lag time and first order elimination. A high absorption rate constant (K01, 4.51/h) signifies that CRM-LF ensured rapid absorption of the CRM into the central compartment. This was followed by the distribution of CRM from the central to peripheral compartment (K12, 2.69/h). The rate of CRM transfer from the peripheral to central compartment (K21, 0.15/h) was slow. This encourages higher tissue levels of CRM as compared with plasma levels. The study provides an explanation of the therapeutic efficacy of CRM, despite very low/undetectable levels in the plasma.http://www.mdpi.com/1999-4923/4/4/517curcuminbioavailabilityabsorptionpharmacokinetic modeling
spellingShingle Arvind K. Bansal
Gunjan Kohli
Jyoti K. Paliwal
Manoj Karwa
Bhushan Munjal
Saurabh Arora
Yogesh B. Pawar
Bioavailability of a Lipidic Formulation of Curcumin in Healthy Human Volunteers
Pharmaceutics
curcumin
bioavailability
absorption
pharmacokinetic modeling
title Bioavailability of a Lipidic Formulation of Curcumin in Healthy Human Volunteers
title_full Bioavailability of a Lipidic Formulation of Curcumin in Healthy Human Volunteers
title_fullStr Bioavailability of a Lipidic Formulation of Curcumin in Healthy Human Volunteers
title_full_unstemmed Bioavailability of a Lipidic Formulation of Curcumin in Healthy Human Volunteers
title_short Bioavailability of a Lipidic Formulation of Curcumin in Healthy Human Volunteers
title_sort bioavailability of a lipidic formulation of curcumin in healthy human volunteers
topic curcumin
bioavailability
absorption
pharmacokinetic modeling
url http://www.mdpi.com/1999-4923/4/4/517
work_keys_str_mv AT arvindkbansal bioavailabilityofalipidicformulationofcurcumininhealthyhumanvolunteers
AT gunjankohli bioavailabilityofalipidicformulationofcurcumininhealthyhumanvolunteers
AT jyotikpaliwal bioavailabilityofalipidicformulationofcurcumininhealthyhumanvolunteers
AT manojkarwa bioavailabilityofalipidicformulationofcurcumininhealthyhumanvolunteers
AT bhushanmunjal bioavailabilityofalipidicformulationofcurcumininhealthyhumanvolunteers
AT saurabharora bioavailabilityofalipidicformulationofcurcumininhealthyhumanvolunteers
AT yogeshbpawar bioavailabilityofalipidicformulationofcurcumininhealthyhumanvolunteers