2. Academic Validation
  3. Inclusion complex between β-cyclodextrin and hecogenin acetate produces superior analgesic effect in animal models for orofacial pain

Inclusion complex between β-cyclodextrin and hecogenin acetate produces superior analgesic effect in animal models for orofacial pain

  • Biomed Pharmacother. 2017 Sep;93:754-762. doi: 10.1016/j.biopha.2017.06.091.
Yasmim M B G Carvalho 1,  Paula P Menezes 2,  Bruna M H Sousa 3,  Bruno S Lima 4,  Igor A S Trindade 5,  Mairim R Serafini 6,  Erik W M Pereira 7,  Marilia M Rezende 8,  Jullyana S S Quintans 9,  Lucindo J Quintans-Júnior 10,  Celso V Nakamura 11,  Edeildo F Silva-Júnior 12,  Alessandre C Crispim 13,  Thiago M Aquino 14,  Adriano A S Araújo 15
Affiliations

Affiliations

  • 1 Department of Pharmacy, Federal University of Sergipe, São Cristóvão, Sergipe, Brazil. Electronic address: [email protected].
  • 2 Department of Pharmacy, Federal University of Sergipe, São Cristóvão, Sergipe, Brazil. Electronic address: [email protected].
  • 3 Department of Pharmacy, Federal University of Sergipe, São Cristóvão, Sergipe, Brazil. Electronic address: [email protected].
  • 4 Department of Pharmacy, Federal University of Sergipe, São Cristóvão, Sergipe, Brazil. Electronic address: [email protected].
  • 5 Department of Pharmacy, Federal University of Sergipe, São Cristóvão, Sergipe, Brazil. Electronic address: [email protected].
  • 6 Department of Pharmacy, Federal University of Sergipe, São Cristóvão, Sergipe, Brazil. Electronic address: [email protected].
  • 7 Department of Physiology, Federal University of Sergipe, São Cristóvão, SE, Brazil,. Electronic address: [email protected].
  • 8 Department of Physiology, Federal University of Sergipe, São Cristóvão, SE, Brazil,. Electronic address: [email protected].
  • 9 Department of Physiology, Federal University of Sergipe, São Cristóvão, SE, Brazil,. Electronic address: [email protected].
  • 10 Department of Physiology, Federal University of Sergipe, São Cristóvão, SE, Brazil,. Electronic address: [email protected].
  • 11 Department of Basic Sciences, State University of Maringa, Maringá, Paraná, Brazil,. Electronic address: [email protected].
  • 12 Laboratory of Nuclear Magnetic Resonance, Institute of Chemistry and Biotechnology, Federal University of Alagoas, Maceió, Alagoas, Brazil. Electronic address: [email protected].
  • 13 Laboratory of Nuclear Magnetic Resonance, Institute of Chemistry and Biotechnology, Federal University of Alagoas, Maceió, Alagoas, Brazil. Electronic address: [email protected].
  • 14 Laboratory of Nuclear Magnetic Resonance, Institute of Chemistry and Biotechnology, Federal University of Alagoas, Maceió, Alagoas, Brazil. Electronic address: [email protected].
  • 15 Department of Pharmacy, Federal University of Sergipe, São Cristóvão, Sergipe, Brazil. Electronic address: [email protected].
PMID: 28704800 DOI: 10.1016/j.biopha.2017.06.091
Abstract

Hecogenin acetate (HA) is a steroidal sapogenin-acetylated with pharmacological properties which have already been described in the literature such as, anti-inflammatory, anti-hyperalgesic and antinociceptive, but it has low solubility in aqueous media. Therefore, in an attempt to overcome this, we set out to create inclusion complexes between HA and b-cyclodextrin (b-CD) and evaluate the antinociceptive effects in the orofacial nociception in mice. The complexes were prepared using different methods in the molar ratios 1:1 and 1:2 and characterized physicochemically. The results of the physicochemical characterization elucidated inclusion complexes formation between b-CD and HA by freeze drying method in the molar ratio 1:2, which obtained a complexation efficiency of 92% and produced superior analgesic effect in animal models for orofacial pain at a lower dose when compared to HA alone.

Keywords

Antinociception; Cyclodextrin; Opioid; Steroidal sapogenin; pain.

Figures
Products