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In order to explore the relationship between the pharmacokinetic properties and pharmacological actions of lipophilic drugs injected with lipid carrier systems, probucol was selected as a model drug with high lipophilicity, and the effect of disposition control on cholesterol-lowering activities was evaluated. Both large emulsion, with mean diameter of 280 nm, and long-circulating type small emulsion containing egg sphingomyelin with mean diameter of 100 nm, showed stable incorporation of probucol. The former produced rapid accumulation of probucol in the liver, while the latter demonstrated prolonged systemic circulation and gradual hepatic uptake. On the other hand, injection of a micellar solution with HCO-60 (polyoxyethylene hydrogenated castor oil) showed a rapid decrease in plasma concentration and a high hepatic uptake of probucol, similar to injections with serum, suggesting the rapid release of the drug from the micelles. However, probucol in a micellar solution showed higher cholesterol-lowering action than that in emulsion formulations. These results suggested that the pharmacological action of probucol in the liver might be affected by the uptake mode and sequential disposition in the organ, depending on the drug retention properties of the lipid carrier particles.

Control of Plasma Cholesterol-Lowering Action of Probucol with Various Lipid Carrier Systems.