Pharmacokinetics, Pharmacodynamics and Drug Metabolism
Bioavailability Enhancement of Curcumin by Complexation with Phosphatidyl Choline

https://doi.org/10.1002/jps.22393Get rights and content

ABSTRACT:

Curcumin is a major constituent of rhizomes of Curcuma longa. Pharmacokinetic studies of curcumin reveal its poor absorption through intestine. Objective of the present study was to enhance bioavailability of curcumin by its complexation with phosphatidyl choline (PC). Complex of curcumin was prepared with PC and characterized on the basis of solubility, melting point, differential scanning calorimetry, thin layer chromatography, and infrared spectroscopic analysis. Everted intestine sac technique was used to study ex vivo drug absorption of curcumin–PC (CU–PC) complex and plain curcumin. Pharmacokinetic studies were performed in rats, and hepatoprotective activity of CU–PC complex was also compared with curcumin and CU–PC physical mixture in isolated rat hepatocytes. Analytical reports along with spectroscopic data revealed the formation of complex. The results of ex vivo study show that CU–PC complex has significantly increased absorption compared with curcumin, when given in equimolar doses. Complex showed enhanced bioavailability, improved pharmacokinetics, and increased hepatoprotective activity as compared with curcumin or CU–PC physical mixture. Enhanced bioavailability of CU–PC complex may be due to the amphiphilic nature of the complex, which greatly enhance the water and lipid solubility of the curcumin. The present study clearly indicates the superiority of complex over curcumin, in terms of better absorption, enhanced bioavailability, and improved pharmacokinetics.

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)

  • P. Anand et al.

    Bioavailability of curcumin: Problems and promises

    Mol Pharm

    (2007)
  • A. Sharma et al.

    Complexation with phosphatidyl choline as a strategy for absorption enhancement of boswellic acid

    Drug Deliv

    (2010)
  • E. Bombardelli et al.

    Complexes between phospholipids and vegetal derivatives of biological interest. Fitoterapia

    (1989)
  • Cited by (0)

    View full text