Enhanced intestinal absorption of daidzein by borneol/menthol eutectic mixture and microemulsion

AAPS PharmSciTech. 2011 Dec;12(4):1044-9. doi: 10.1208/s12249-011-9672-4. Epub 2011 Aug 13.

Abstract

In the present study, the effect of a borneol/menthol eutectic mixture (25:75) and microemulsion on the absorption of daidzein in rat intestinal membrane was evaluated. The microemulsion formulation was composed of ethyl oleate (oil), Cremophor RH40 (surfactant), PEG400 (co-surfactant), and water. The borneol/menthol eutectic mixture and its microemulsion were found to enhance the intestinal absorption of daidzein in vitro. A diffusion chamber system with isolated rat intestinal membranes was used. In contrast, verapamil (0.3 mM), a typical P-glycoprotein inhibitor, showed no effect on the absorption of daidzein by this system. A pharmacokinetic study was conducted in rats. After oral administration of daidzein at a dose of 10 mg/kg in the form of either borneol/menthol eutectic mixtures or suspension, the relative bioavailability of borneol/menthol eutectic mixtures and microemulsion was enhanced by about 1.5- and 3.65-fold, respectively, compared with a daidzein suspension. In conclusion, a borneol/menthol eutectic mixture can enhance the absorption of daidzein, although the mechanism of absorption enhancement is still unclear.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • ATP Binding Cassette Transporter, Subfamily B, Member 1 / antagonists & inhibitors
  • ATP Binding Cassette Transporter, Subfamily B, Member 1 / metabolism
  • Administration, Oral
  • Animals
  • Biological Availability
  • Camphanes / administration & dosage
  • Camphanes / chemistry
  • Camphanes / pharmacology*
  • Chemistry, Pharmaceutical
  • Dose-Response Relationship, Drug
  • Drug Compounding
  • Emulsions
  • Intestinal Absorption / drug effects*
  • Intestinal Mucosa / metabolism
  • Intestines / drug effects*
  • Isoflavones / administration & dosage
  • Isoflavones / chemistry
  • Isoflavones / pharmacokinetics*
  • Male
  • Methanol / administration & dosage
  • Methanol / chemistry
  • Methanol / pharmacology*
  • Oils / chemistry
  • Oleic Acids / chemistry
  • Polyethylene Glycols / chemistry
  • Rats
  • Rats, Sprague-Dawley
  • Solubility
  • Surface-Active Agents / chemistry
  • Technology, Pharmaceutical
  • Verapamil / pharmacology
  • Water / chemistry

Substances

  • ATP Binding Cassette Transporter, Subfamily B, Member 1
  • Camphanes
  • Emulsions
  • Isoflavones
  • Oils
  • Oleic Acids
  • Surface-Active Agents
  • Water
  • cremophor
  • Polyethylene Glycols
  • daidzein
  • Verapamil
  • isoborneol
  • Methanol
  • ethyl oleate