Pharmacokinetic Characterization of Nano-emulsion Vitamin A, D and E (LaVita) in Rats

Lee, Young-Ju;Kwon, Min;Kim, Tae-Hwan;Kim, Kyun;Jeong, Sang-Hee;Chang, Hee-Ra

  • 투고 : 2011.06.01
  • 심사 : 2011.06.24
  • 발행 : 2011.06.30


BACKGROUND: Bioavailability enhancement by solubilization of lipophilic drugs in nano-emulsion has been reported and it may be useful in pharmaceutical and nutraceutical products. This study was performed to compare in vivo bioavailability of nano-emulsion formulation with that of the general product as control. METHODS AND RESULTS: The pharmacokinetics assessment of Vitamin A, D and E complex of nanoemulsion formulation (LaVita), in comparison to the general product, was performed in the male rat plasma by a single oral dose at 20 mL/kg body weight (n=3/group). For nano-emulsion formulation (LaVita), $C_{max}$ of vitamin A and E in plasma were much higher and the area under the curve (AUC) of vitamin A, D and E were 14-63% higher, and the half-life of vitamin E was 2-fold longer than the general product. According to statistical analysis, each $C_{max}$ of vitamin A, D & E was significantly higher (p<0.01, 0.05 and 0.01, respectively) than that of general product. Half-life of vitamin A was significantly higher (p<0.01) and AUC of vitamin A and D were also significantly higher than the general product. CONCLUSION(s): Considering significant increment of $C_{max}$ and AUC, LaVita made of nano-emulsion could be more effective the absorption rate and extent for bioavailability of vitamin A, D & E than those of general product.


Bioavailability;Fat-soluble vitamin;Nanoemulsion;Pharmacokinetics;Plasma


  1. Brusewitz, C., Schendler, A., Funke, A., Wagner, T., Lipp, R., 2007. Novel poloxamer-based nanoemulsions to enhance the intestinal absorption of active compounds, Int. J. Pharm. 329, 173-181.
  2. Burton, G.W., Ingold, K.U., Foster, D.O., Cheng, S.C., Webb, A., Hughes, L., Lusztyk, Ewa., 1988. Comparison of free $\alpha$-Tocopherol and $\alpha$-Tocopheryl Acetate as Sources of Vitamin E in Rats and Humans, Lipid 23, 834-840.
  3. Burton, G.W., Traber, M.G., 1990. Vitamin E: Antioxidant activity, Biokinetics, and Bioavailability, Annu. Rev. Nutr. 10, 357-382.
  4. Gomis, D,B,, Escotet, A.V.J., Fidalgo, A.L.E., Gutierrez, A.M.D., 1994. Simulataneous determination of vitamins D3, E and K1 and retinyl palmitate in cattle plasma by liquid chromatography with a narrow- bore column, J. Chromatogr. B 660, 49-55.
  5. Gonzalez, M.J., 1990. Serum Concentrations and Cellular Uptake of Vitamin E, Med. Hypotheses 32, 107-110.
  6. Gutierrez, J.M., Gonzalez, C., Maestro, A., Sole, I., Pey, C.M., Nolla, J., 2008. Nano-emulsions: New applications and optimization of their preparation. Curr. Opin. Coll. Int. Sci. 13, 245-251.
  7. Hatanaka, J., Chikamori, H., Sato, H., Uchida, S., Debari, K., Onoue, S., Yamada, S., 2010. Physicochemical and pharmacological characterization of $\alpha$-tocopherol-loaded nano-emulsion syatem. Int. J. Pharm. 396, 188-193.
  8. Hidiroglou, M., Ivan, M., Toutain, P.L., 1994. Metabolism of Tritiated D-$\alpha$-Tocopherol and D-$\alpha$ -Tocophery Succinate in Intraruminally Dosed Sheep. J. Anim. Sci. 72, 2124-2130.
  9. Heudi, O., Trisconi, M.J., Blake, C.J., 2004. Simultaneous quantification of Vitamins A, D3, and E in fortified infant formulae by liquid chromatography- mass spectrometry. J. Chromatogr. A 1022, 115-123.
  10. Kang, H.S., Kwon, S.S., Kim, B.H., Lee, B.R., Kang, K.H., Hong, J.E., Han, S.H., Chang, I.S., 2002. Nanoemulsion as a Vitamin E Acetate Carrier to Enhance Infiltration into Oral Mucous Membrane, J. Ind. Eng. Chem. 8, 348-353.
  11. Lee, S.J., Choi, S.J., Li, Y., Decker, E.A., 2011. McClements DJ. Protein-Stabilized Nanoemulsions and Emulsions: Comparison of Physicochemical Stability, Lipid Oxidation, and Lipase Digestibility, J. Agric. Food. Chem. 59, 415-427.
  12. Mendoza, B.R., Pons, S.M., Bargallo, A.I.C., Lopez-Sabater, M.C., 2003. Rapid determination by reversed-phase high-performance liquid chromatography of Vitamin A and E in infant formulas, J. Chromatogr. A 1018, 197-202.
  13. Solans, C., Izquierdo, P., Nolla, J., Azemar, N., Garcia-Celma, M.J., 2005. Nano-emulsion, Curr. Opin. Coll. Int. Sci. 10, 102-110.
  14. Tadros, T., Izquierdo, P., Esquena, J., Solans, C., 2004. Formation and stability of nano-emulsions, Adv. Colloid. Interface. Sci. 108-109, 303-318.
  15. Taha, E., Ghorab, D., Zaghloul, A.A., 2007. Bioavailability Assessment of Vitamin A Self-Nanoemulsified Drug Delivery Systems in Rats: A Comparative Study, Med, Princ, Pract. 16, 355-359.

피인용 문헌

  1. Nanoemulsions for food fortification with lipophilic vitamins: Production challenges, stability, and bioavailability vol.119, pp.7, 2017,


연구 과제 주관 기관 : Hoseo University