Carriers for skin delivery of trihexyphenidyl HCl: ethosomes vs. liposomes

Biomaterials. 2000 Sep;21(18):1879-85. doi: 10.1016/s0142-9612(00)00063-6.

Abstract

The purpose of this work was to characterize a novel ethosomal carrier containing trihexyphenidyl HCl (THP) and to investigate the delivery of THP from ethosomes versus classic liposomes. THP-ethosomal systems were shown by electron microscopy to contain small, phospholipid vesicles. As the THP concentration was increased from 0 to 3%, the size of the vesicles decreased from 154 to 90 nm. This is most likely due to the surface activity of THP (critical micelle concentration of 5.9 mg/ml), as measured in this work. In addition, the ethosome zeta potential value increased as a function of THP concentration, from -4.5 to +10.4 when the THP concentration was increased from 0 to 3%. In contrast, THP liposomes were much larger and their charge was not affected by THP. When compared with standard liposomes, ethosomes had a higher entrapment capacity and a greater ability to deliver entrapped fluorescent probe to the deeper layers of skin. The flux of THP through nude mouse skin from THP ethosomes (0.21 mg/cm2 h) was 87, 51 and 4.5 times higher than from liposomes, phosphate buffer and hydroethanolic solution, respectively (p < 0.01). The quantity of THP remaining in the skin at the end of the 18-h experiment was statistically significantly greater from the ethosomal system than from liposomes or a control hydroethanolic solution. Our results indicate that the ethosomal THP system may be a promising candidate for transdermal delivery of THP.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Calorimetry, Differential Scanning
  • Drug Carriers*
  • Drug Stability
  • Injections, Intradermal*
  • Kinetics
  • Liposomes*
  • Mice
  • Mice, Nude
  • Micelles
  • Microscopy, Electron
  • Microscopy, Electron, Scanning
  • Phosphatidylcholines* / chemistry
  • Skin / metabolism*
  • Trihexyphenidyl / administration & dosage*
  • Trihexyphenidyl / pharmacokinetics

Substances

  • Drug Carriers
  • Liposomes
  • Micelles
  • Phosphatidylcholines
  • Trihexyphenidyl