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. Epub 2017 Jul 10.

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.

MeSH terms

  • Analgesics / chemistry*
  • Analgesics / pharmacology*
  • Animals
  • Drug Compounding / methods
  • Facial Pain / drug therapy*
  • Freeze Drying / methods
  • Male
  • Mice
  • Models, Animal
  • Solubility
  • Spiro Compounds / chemistry*
  • Spiro Compounds / pharmacology*
  • Steroids / chemistry*
  • Steroids / pharmacology*
  • beta-Cyclodextrins / chemistry*
  • beta-Cyclodextrins / pharmacology*

Substances

  • Analgesics
  • Spiro Compounds
  • Steroids
  • beta-Cyclodextrins
  • hecogenin acetate