Non-ionic surfactants and membrane transport of thioridazine in goldfish

Abstract

Polysorbate 80, which has been widely used in studies of the effects of surfactants on drug absorption, increases the rate of absorption of some drugs at concentrations near its critical micelle concentration (cmc). To determine whether all non-ionic surfactants were capable of inducing this effect, the effects of six commercial non-ionic surfactants on thioridazine absorption in goldfish have been compared with the effect of polysorbate 80. The reciprocal death time (T−1) determined when the fish were immersed in the solution under study was the index of absorption rate used. Not all surfactants tested increased T−1. Cremophor EL (polyoxyethylated castor oil), Atlas G1295 (a polyoxyethylene fatty glyceride), Atlas G1300 (a polyoxyethylene glyceride ester) had no effect below their cmc’s. Those surfactants that did increase T−1 [polysorbate 80 (a polyoxyethylene sorbitan monooleate), Atlas G1790 (a polyoxyethylene lanolin derivative), G2162 (a polyoxyethylene oxypropylene monostearate) and Renex 650 (a polyoxyethylene alkyl aryl ether)] display the concentration-dependent behaviour reported previously–a decrease in absorption rate when the surfactant concentration is increased above its cmc. The factor determining whether or not the surfactant will increase absorption rate appears to be the configuration of the surfactant molecule rather than its hydrophile-lipophile balance or its surface activity.