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Formulation development and in vivo hepatoprotective activity of self nanoemulsifying drug delivery system of antioxidant coenzyme Q10

Abstract

Coenzyme Q10 (CQ10) is known as an endogenous cellular antioxidant, naturally found in every cell of the human body and plays an important role in maintaining human health. It is widely used as a nutritional supplement and pharmaceutical drug for various disorders like diabetes mellitus, carcinomas, neurodegenerative disorders etc. However, CQ10 is practically insoluble even in the presence of 5 % sodium lauryl sulfate in water and poorly absorbed from the gastrointestinal tract. The present research is aimed to formulate and evaluate self nanoemulsifying drug delivery system (SNEDDS) of CQ10 primarily to improve its aqueous solubility, dissolution velocity as well as hepatoprotective activity and thus enhancing its nutraceutical and pharmaceutical values. Robustness to dilution, thermodynamic stability study, droplet size analysis and drug release were adopted to optimize liquid SNEDDS. Droplet size of the SNEDDS was found to be size less than 200 nm and appeared round in shape without aggregation under transmission electron microscopy examination. Liquid SNEDDS were adsorbed on porous carrier to get solid SNEDDS (S-SNEDDS). S-SNEDDS gave rapid (>90 %) drug release within 30 min while pure drug was not practically dissolved within 1 h. In vivo hepatoprotective activity showed that S-SNEDDS achieved the most liver protection as compared to the pure drug. Further S-SNEDDS was successfully converted to self nanoemulsifying mouth dissolving tablet. The enhanced solubility, dissolution velocity as well as hepatoprotective activity of CQ10, unravels the potential of S-SNEDDS as suitable carrier for enhancing nutraceutical and pharmaceutical values of CQ10.

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Acknowledgments

The author Anuj G. Agrawal wish to thank Mr. S. K. Singh (Director) and Mr. Sanjay Kumar (VPFO), Cachet Pharmaceutical Pvt. Ltd., India for providing the necessary facilities and Dr. Pralhad Wangikar (CEO), PRADO Preclinical Research and Development Organization Pvt. Ltd., India for assistance in conduct of in vivo hepatoprotective activity.

Conflict of interest

We have no personal relationships with other people or organizations that could inappropriately influence the presented work or any affiliation with any organization with a financial interest, direct or indirect, in the subject matter or materials discussed in the manuscript.

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Agrawal, A.G., Kumar, A. & Gide, P.S. Formulation development and in vivo hepatoprotective activity of self nanoemulsifying drug delivery system of antioxidant coenzyme Q10 . Arch. Pharm. Res. (2014). https://doi.org/10.1007/s12272-014-0497-z

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Keywords

  • Coenzyme Q10
  • SNEDDS
  • Antioxidant
  • Solubility
  • Dissolution
  • Nanoemulsion