Pharmacokinetics, Pharmacodynamics and Drug MetabolismBioavailability Enhancement of Curcumin by Complexation with Phosphatidyl Choline
Section snippets
INTRODUCTION
Curcumin, a natural polyphenol, found in the rhizomes of Curcuma longa (turmeric), which is used as a spice and food coloring in Indian cooking, is well known for its medicinal properties since ancient times. Curcumin shows antioxidant activity as seen by its ability to inhibit lipid peroxidation. The antioxidant activity of curcumin arises mainly from scavenging of several biologically relevant free radicals that are produced during physiological processes. Apart from antioxidant action,
Materials
Curcumin and cholesterol(Sigma-Aldrich, St. Louis, MO) were purchased from USA. The soy phosphatidyl choline (PC) (Lipoid S 100) was obtained as gift sample from Lipoid, Ludwigshafen, Germany. All other chemicals and solvents were of analytical grade.
Preparation of CU–PC Complex
Curcumin and soy PC in molar ratio of 1:1 were taken in a round bottom flask and dissolved in 20 mL of dichloromethane. This mixture was refluxed for 2 h at room temperature on a magnetic stirrer. The solvent was then removed under reduced pressure
Solubility Study
As shown in Table 1, the CU–PC complex has different solubility profile than plain curcumin, which indicates the formation of complex.
Differential Scanning Calorimetry
Interaction of drug with excipient can be examined by DSC, which also gives information about compatibility of drug with excipient. In DSC, an interaction is concluded by elimination of endothermic peaks, appearance of new peaks, change in peak shape and its onset, peak temperature/melting point, and relative peak area. DSC thermograms of curcumin, PC, and CU–PC
DISCUSSION
Phytomedicines, complex chemical mixtures prepared from plants, have been used for health maintenance since ancient times. But many phytomedicines are limited in their effectiveness because they are poorly absorbed when taken by mouth. The recent trend is to improve the therapeutic performance of the conventional drug by formulating them as new drug delivery system rather than going for cumbersome and costly research for a new entity.10., 11., 12.
The effectiveness of any herbal product is
CONCLUSION
In the present work, complex of curcumin was prepared with PC to enhance the bioavailability of curcumin. The prepared complex was characterized and evaluated in terms of absorption through intestine, pharmacokinetic studies, and hepatoprotective potential. The results of present study clearly indicate the superiority of CU–PC complex over plain curcumin or CU–PC physical mixture, in terms of better absorption, enhanced bioavailability, and improved pharmacokinetics.
ACKNOWLEDGEMENTS
The authors thank LIPOID GmbH (Germany) for providing the gift sample of phosphatidyl choline. The authors also acknowledge the Council of Scientific and Industrial Research (CSIR), New Delhi, India, for providing financial assistance (grant no. 09/150/(0100)/2009/EMR-I) in the form of Senior Research Fellowship to Nishant Kumar Gupta.
REFERENCES (26)
- et al.
Curcumin: The story so far
Eur J Cancer
(2005) - et al.
Studies of curcumin and curcuminoids. XXVII. Cyclodextrin complexation: Solubility, chemical and photochemical stability
Int J Pharm
(2002) - et al.
Curcumin for chemoprevention of colon cancer
Cancer Lett
(2007) - et al.
Enhancement of oral absorption of curcumin by self-microemulsifying drug delivery systems
Int J Pharm
(2009) - et al.
The preparation of silybin-phospholipid complex and the study on its pharmacokinetics in rats
Int J Pharm
(2006) - et al.
In vitro studies on the intestinal absorption of curcumin in rats
Toxicology
(1981) - et al.
Anticancer potential of curcumin: Preclinical and clinical studies
Anticancer Res
(2003) - et al.
Biotransformation of curcumin through reduction and glucuronidation in mice
Drug Metab Dispos
(1999) - et al.
Phase I clinical trial of oral curcumin: Biomarkers of systemic activity and compliance
Clin Cancer Res
(2004) - et al.
Comparison of systemic availability of curcumin with that of curcumin formulated with phosphatidyl choline
Cancer Chemother Pharmacol
(2007)