[Amphiphilic drugs. 2. Relation between colloidal properties and pharmaceutic-technological, pharmacokinetic and...

The physicochemical properties of amphiphilic drugs may affect the technological, pharmacokinetic and pharmacodynamic behaviours. Micelle formation of a drug is of considerable importance for its solubility, stability, adsorption pattern, mixed micelle formation and influences thus its pharmaceutical availability. The biological availability is in many cases decreased by interactions of a surface active drug with other substances before absorption, by altered diffusion behaviour and distribution properties. Colloidal association may also result in an alteration of pharmacodynamic effects. These relations depend on the fact, that discrete hydrophobic an hydrophilic parts in a molecule are also prerequisites for micelle formation and receptor interactions. Furthermore the high membrane affinity of these drugs is responsible for some therapeutic and toxic effects.