Abstract
Purpose. To measure the effect of a combination of excipients from a silicone based pressure sensitive adhesive (PSA) on drug transport across skin.
Methods. Partitioning of propylene glycol monolaurate (PG-ML) from silicone PSA and a solution formulation into the stratum corneum (SC) was measured using radiolabeled PG-ML. Transport of a model drug, estradiol, as well as PG-ML across skin were measured in vitro using heat separated epidermis from human cadaver skin.
Results. The PG-ML partitioning into SC showed a saturation and was independent of the formulation. The local dielectric of the lipid bilayers of the SC showed an increase as a result of PG-ML uptake, as determined by the decrease in fluorescence lifetime of a lipophilic probe incorporated into the SC. However, there was no alteration of lipid packing in SC.
Conclusions. The PG-ML and estradiol transport showed a good correlation over 3 days, suggesting that the two species are co-transported across the epidermis.
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Irion, G.D., Garrison, M.D. & Abraham, W. Effect of PGML Excipient Mixture in a Transdermal System on the in Vitro Transport of Estradiol Across Skin. Pharm Res 12, 1618–1622 (1995). https://doi.org/10.1023/A:1016232831431
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DOI: https://doi.org/10.1023/A:1016232831431