The effect of component of microemulsions on transdermal delivery of buspirone hydrochloride

J Pharm Sci. 2011 Jun;100(6):2358-65. doi: 10.1002/jps.22474. Epub 2011 Jan 18.

Abstract

The aim of this study was to evaluate the influence of components such as type, level, and hydrophilic-lipophilic balance (HLB) value of surfactant, type and amount of cosurfactant, and drug concentration on the permeability of buspirone hydrochloride microemulsions through rat skin. The cumulative amount at 24 h ranged from 502.2 ± 57.8 to 1754.3 ± 616.6 μg/cm(2), flux ranged from 23.03 ± 1.84 to 83.36 ± 25.08 μg/(cm(2)/h), and lag time ranged from 3.0 to 4.7 h, indicating that the permeation parameters of buspirone from microemulsions were markedly influenced by the composition of microemulsions. In comparison with the effect of composition of microemulsions on the buspirone permeation capacity, it was found that microemulsions containing surfactant with HLB value of 11.16 possessed higher flux. The viscosity of microemulsions increased, flux decreased, and lag time was prolonged when amount of surfactant in microemulsions increased. The various cosurfactants can also influence the microemulsion formation and drug permeability. The microemulsion with ethanol as cosurfactant had higher permeation rate. However, the buspirone microemulsion with higher flux can provide the therapeutic minimum effective concentration, at workable administrated area about 3.3-5.8 cm(2), demonstrating microemulsions could be a promising drug carrier for transdermal delivery systems.

MeSH terms

  • Administration, Cutaneous
  • Animals
  • Anti-Anxiety Agents / administration & dosage*
  • Buspirone / administration & dosage*
  • Chromatography, High Pressure Liquid
  • Drug Carriers / chemistry*
  • Emulsions
  • Female
  • Hydrophobic and Hydrophilic Interactions
  • In Vitro Techniques
  • Particle Size
  • Permeability
  • Rats
  • Rats, Sprague-Dawley
  • Skin / metabolism*
  • Skin Absorption / drug effects
  • Solubility
  • Time Factors
  • Viscosity

Substances

  • Anti-Anxiety Agents
  • Drug Carriers
  • Emulsions
  • Buspirone