Effect of PGML excipient mixture in a transdermal system on the in vitro transport of estradiol across skin

Pharm Res. 1995 Nov;12(11):1618-22. doi: 10.1023/a:1016232831431.

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.

MeSH terms

  • Administration, Cutaneous
  • Estradiol / administration & dosage
  • Estradiol / chemistry
  • Estradiol / pharmacokinetics*
  • Excipients / pharmacology*
  • Humans
  • In Vitro Techniques
  • Laurates / pharmacology*
  • Propylene Glycols / pharmacology*
  • Silicones / chemistry
  • Silicones / pharmacology
  • Skin / chemistry
  • Skin Absorption / drug effects*
  • Spectrometry, Fluorescence
  • Thermodynamics
  • Tissue Adhesives

Substances

  • Excipients
  • Laurates
  • Propylene Glycols
  • Silicones
  • Tissue Adhesives
  • propyleneglycol monolaurate
  • Estradiol