Haemolytic activity of maltopyranoside surfactants.
The haemolytic activity of a number of maltopyranoside surfactants was studied. The study included octyl, nonyl, decyl, dodecyl, tetradecyl, cyclohexyl-propyl, cyclohexyl-hexyl, and dimethyl-heptyl maltopyranoside. The in vitro haemolytic activity was determined by employing a static method in which surfactants are added to an erythrocyte suspension and the released haemoglobin is determined. It was found that alkyl maltopyranosides become more haemolytic the longer the alkyl chain. Branching or presence of cyclic groups clearly decreases haemolytic activity, but it also increases the critical micelle concentration. As a result, the cyclic or branched surfactants do not become better solubilizing excipients than the straight-chain surfactants. The most useful surfactant for pharmaceutical applications appears to be tetradecyl maltopyranoside, which is the least haemolytic surfactant relative to its critical micelle concentration.
Söderlind
Erik
E
AstraZeneca R&D Mölndal, Mölndal, Sweden. erik.soderlind@astrazeneca.com
Karlsson
Lina
L
D000328:Adult; D000465:Algorithms; D002240:Carbohydrate Sequence; D006461:Hemolysis / Q000187:drug effects*; D006801:Humans; D066298:In Vitro Techniques; D008320:Maltose / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology*; D008969:Molecular Sequence Data; D013329:Structure-Activity Relationship; D013501:Surface-Active Agents / Q000737:chemistry / Q000494:pharmacology*
D013501:Surface-Active Agents; D008320:Maltose