VEHICLE EFFECTS ON IN-VITRO SKIN PERMEATION OF AND STRATUM-CORNEUM AFFINITY FOR MODEL-DRUGS CAFFEINE AND TESTOSTERONE

The effects of Labrasol (LBS) (glycolysed ethoxylated C-8/C-10 glycerides), Labrafil (LBF) (glycolysed ethoxylated glycerides), Transcutol (TSC) (diethylene glycol monoethyl ether) and DPPG (propylene glycol dipelargonate) on the flux across excised human skin of the lipophilic testosterone (TST) and the hydrophilic caffeine (CAF) and on the affinity of the human stratum corneum for these drugs are compared taking propylene glycol (PG) and liquid petrolatum (LP) as reference vehicles. DPPG and LBF enhance CAF flux relative to PG while LBS and TSC increase the stratum corneum affinity for TST relative to LP. However, the materials tested enhance neither the flux of nor the stratum corneum affinity for both drugs with respect to either reference. On the other hand, a saturated solution of DPPG in PG enhances both properties for both drugs relative to PG. Such effects are ascribed to the ability of DPPG to interact with the lipid bilayers and to that of PG to promote DPPG penetration into stratum corneum and to create interaction sites in such a tissue.