Transdermal iontophoretic peptide delivery: in vitro and in vivo studies with luteinizing hormone releasing hormone.
Protein and peptide drugs are not orally active. Their large molecular size and charged character make them poor candidates for passive transdermal delivery. With an applied electromotive force, these drugs can be forced through the skin to be absorbed by the systemic circulation. The present study investigates the transdermal iontophoretic delivery of a peptide hormone in an in vitro model system, the isolated perfused porcine skin flap, as well as in vivo. It is shown that with knowledge of the systemic disposition of the drug, transdermal fluxes can be utilized to accurately predict in vivo serum concentrations. It is also shown that the iontophoretically delivered hormone retains both its immunologic and biologic activity.
Heit
M C
MC
Cutaneous Pharmacology and Toxicology Center, North Carolina State University, Raleigh 27606.
Williams
P L
PL
Jayes
F L
FL
Chang
S K
SK
Riviere
J E
JE
D000279:Administration, Cutaneous; D000818:Animals; D005260:Female; D005640:Follicle Stimulating Hormone / Q000097:blood; D007987:Gonadotropin-Releasing Hormone / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics; D007275:Injections, Intravenous; D007478:Iontophoresis; D007986:Luteinizing Hormone / Q000097:blood; D011863:Radioimmunoassay; D013552:Swine
D007987:Gonadotropin-Releasing Hormone; D007986:Luteinizing Hormone; D005640:Follicle Stimulating Hormone