Dj. Pillion et al., ALKYLGLYCOSIDES ENHANCE SYSTEMIC ABSORPTION OF INSULIN APPLIED TOPICALLY TO THE RAT EYE, The Journal of pharmacology and experimental therapeutics, 271(3), 1994, pp. 1274-1280
A series of alkylglycosides with various alkyl chain lengths and carbo
hydrate residues were tested for their ability to enhance systemic abs
orption of insulin after topical ocular delivery in anesthetized rats.
Several reagents, including tetradecyl-, tridecyl- and dodecylmaltosi
de and dodecylsucrose, were potent stimulators of insulin absorption w
hen used at concentrations as low as 0.125%. Other alkylglycosides suc
h as decylsucrose, decylmaltoside, nonylglucoside, octylmaltoside, hep
tylglucoside and hexylglucoside were less potent or ineffective as abs
orption-enhancing reagents. By comparison, the bile salt sodium glycoc
holate was effective only when used at concentrations of 0.5% or great
er. All of the reagents were effective only when used at concentration
s above their critical micelle concentration and the most hydrophobic
alkylglycoside reagents were the most efficacious at promoting systemi
c insulin absorption. The possible utilization of eyedrops containing
insulin plus an absorption-enhancing alkylglycoside reagent in humans
is discussed.