Lecithin organogel as matrix for transdermal transport of drugs.
Organogels obtained by adding small amounts of water to a solution of lecithin in organic solvents were studied as matrices for the transdermal transport of drugs. Gels obtained from isopropyl palmitate and cyclooctane were used (molar ratios of water to lecithin of 3 and 12, respectively). Preliminarily histological studies showed that the gels have no harmful effect when applied to the skin for prolonged periods. Data relative to the stability of the organogels with time are also presented. Scopolamine and broxaterol were used as model drugs, and the transdermal experiments were done with a Franz diffusion cell and human skin obtained from plastic surgery. The transport rate of scopolamine obtained with the lecithin gels was about one order of magnitude higher than that obtained with an aqueous solution of the drug at the same concentration. In contrast, the transport rates of scopolamine obtained with the microemulsion solution prior to gelation (molar ratio of water to lecithin, 0) were not different from those obtained with the gel. The same variations in transport rates were observed for broxaterol, in which case the flux through the skin was directly proportional to the concentration of drug in the gel. At a concentration of broxaterol of 75 mg/mL in the donor gel, the flux was 47 micrograms.h-1.cm-2. Because preliminary results showed that transdermal transport is successful with amino acids and peptides also, it is concluded that lecithin gels may be efficient vehicles for the transdermal transport of various drugs.
Willimann
H
H
ETH-Zentrum, Institut für Polymere, Zürich, Switzerland.
Walde
P
P
Luisi
P L
PL
Gazzaniga
A
A
Stroppolo
F
F
D000328:Adult; D001692:Biological Transport; D005260:Female; D005782:Gels; D006801:Humans; D007555:Isoxazoles / Q000008:administration & dosage / Q000493:pharmacokinetics; D014677:Pharmaceutical Vehicles; D010713:Phosphatidylcholines / Q000008:administration & dosage*; D012601:Scopolamine / Q000008:administration & dosage / Q000493:pharmacokinetics; D012869:Skin Absorption
D005782:Gels; D007555:Isoxazoles; D014677:Pharmaceutical Vehicles; D010713:Phosphatidylcholines; D012601:Scopolamine; C045916:broxaterol