Mechanisms of liposomes/water partitioning of (p-methylbenzyl)alkylamines

Pharm Res. 1998 Sep;15(9):1407-13. doi: 10.1023/a:1011953622052.

Abstract

Purpose: The objective of this study was to compare and interpret the variations in lipophilicity of homologous (p-methylbenzyl)alkylamines (MBAAs) in isotropic (octanol/water) and anisotropic (zwitterionic liposomes/water) system.

Methods: Two experimental approaches were used, namely the pH-metric method to measure lipophilicity parameters in octanol/water and liposomes/water systems, and changes in NMR relaxation rates to validate the former method and to gain additional insights into the mechanisms of liposomes/water partitioning.

Results: For long-chain homologues (N-butyl to N-heptyl), the octanol/water and liposomes/water systems mostly expressed hydrophobicity. In contrast, the lipophilicity of the shorter homologues (N-methyl to N-propyl) in the two systems expressed various electrostatic and polar interactions.

Conclusions: The study sheds light on the molecular interactions between zwitterionic liposomes and amphiphilic solutes in neutral and cationic form.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 1-Octanol / chemistry*
  • Alkanes / chemistry*
  • Drug Carriers
  • Lipids / chemistry
  • Liposomes / chemistry
  • Magnetic Resonance Spectroscopy
  • Water / chemistry*

Substances

  • Alkanes
  • Drug Carriers
  • Lipids
  • Liposomes
  • Water
  • 1-Octanol