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Development and in vitro biopharmaceutical evaluation of a dihydroquercetin microemulsion

  • M. V. Karlina
  • O. N. Pozharitskaya
  • A. N. Shikov
Article

Dihydroquercetin (DHQ) is a readily available compound with a broad spectrum of biological activity that makes development of new drug forms based on this compound imperative. In particular, it exhibits capillary-protective, anti-oxidant, and anti-inflammatory effects. Microemulsions are promising systems for delivering drugs and can increase their biological availability and provide their controlled release. A water-in-oil microemulsion containing DHQ (2%), surfactant (Tween 80), cosurfactant (propyleneglycol), an oil phase (Labrafil M 1944 CS), and water was prepared. Physicochemical parameters (particle size, viscosity, refractive index, denisty, and pH) and the in vitro release of DHQ were studied by the paddle-over-disk method in systems modeling local transdermal application and the paddle method in systems modeling oral application. Release rate constants were calculated. The proposed microemulsion ensures uniform prolonged release of the active substance.

Key words

dihydroquercetin microemulsion biopharmaceutical evaluation bioaccessibility 

References

  1. 1.
    T. Yu. Il’yuchenok, A. I. Khomenko, L. M. Frigidova, et al., Farmakol. Toksikol. (Moscow), No. 5, 607–612 (1975).Google Scholar
  2. 2.
    A. A. Kubatiev, Z. T. Yadigarova, I. A. Rud’ko, et al., Vopr. Biol. Med. Farm. Khim., No. 3, 47–51 (1999).Google Scholar
  3. 3.
    V. K. Kolkhir, N. A. Tyukavkina, V. A. Bykov, et al., Khim.-farm. Zh., No. 9, 61–64 (1995).Google Scholar
  4. 4.
    Yu. O. Teselkin, I. V. Babenkova, V. G. Novozhenov, et al., Vopr. Biol. Med. Farm. Khim., No. 1, 36–45 (1999).Google Scholar
  5. 5.
    V. K. Kolhir, V. A. Bykov, A. I. Baginskaja, et al., Phytother. Res., 10, 478–482 (1996).CrossRefGoogle Scholar
  6. 6.
    Y.-S. Rhee, J.-G. Choi, E.-S. Park, et al., Int. J. Pharm., 228, 161–170 (2001).CrossRefPubMedGoogle Scholar
  7. 7.
    P. P. Constantinides, J. P. Scalart, C. Lancaster, et al., Pharm. Res., 11(10), 1385–1390 (1994).CrossRefPubMedGoogle Scholar
  8. 8.
    H. M. El-Laithy, AAPS PharmSciTech, 4(1), Article 11 (2003).Google Scholar
  9. 9.
    P. K. Ghosh, R. J. Majithiya, and M. L. Umrethia, AAPS PharmSciTech, 15, No. 7 (3), Article 77 (2006).Google Scholar
  10. 10.
    H. M. El-Laithy and K. M. F. El-Shaboury, AAPS PharmSciTech, 3(4), Article 35 (2002).Google Scholar
  11. 11.
    B. K. Kang, S. K. Chon, S. H. Kim, et al., Int. J. Pharm., 22; 286(1–2), 147–156 (2004).Google Scholar
  12. 12.
    US Pharmacopoeia, National Formulary, USP 28-NF23 (2005).Google Scholar
  13. 13.
    M. V. Karlina, O. N. Pozharitskaya, and V. M. Kosman, Vopr. Biol. Med. Farm. Khim., 9(3), 42–46 (2006).Google Scholar
  14. 14.
    V. Pillay and R. Fassihi, Pharm. Sci., 88(9), 843–851 (1999).CrossRefGoogle Scholar
  15. 15.
    M. Karlina, O. Pozharitskaya, and A. Shikov, Planta Med., 73(9), 905–906 (2007).CrossRefGoogle Scholar
  16. 16.
    A. N. Shikov, O. N. Pozharitskaya, M. V. Karlina, and V. G. Makarov, Eur. J. Pharm. Sci., 34(1), Suppl. 1, S29 (2008).CrossRefGoogle Scholar
  17. 17.
    M. Siewert, J. Dressman, C. K. Brown, et al., AAPS PharmSciTech, 4(1), Article 7 (2003).Google Scholar
  18. 18.
    W. I. Higuchi, J. Pharm. Sci., 51, 802–804 (1962).CrossRefPubMedGoogle Scholar

Copyright information

© Springer Science+Business Media, Inc. 2009

Authors and Affiliations

  • M. V. Karlina
    • 1
  • O. N. Pozharitskaya
    • 1
  • A. N. Shikov
    • 1
  1. 1.St. Petersburg Institute of PharmacySt. PetersburgRussia

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