Bioadhesive monolayer film for the in vitro transdermal delivery of sumatriptan.
The work presented here aims to develop a bioadhesive monolayer film containing sumatriptan as adjuvant for the treatment of headache pain in a severe migraine attack. Permeation experiments were performed from the films prepared and from the respective solution, to evaluate the relevant permeation parameters. The effect of the penetration enhancers Transcutol, 2-pyrrolidone, and polyethylene glycol 600 was evaluated. The results obtained show that Transcutol and 2-pyrrolidone decreased sumatriptan permeation from solution, whereas a modest increase was produced by polyethylene glycol 600. The enhancers produced the same effects when they were included in the film. Compared to solution, the film showed a higher sumatriptan flux in the early times of the experiment. When the film was applied in occlusive conditions the profiles were much higher, indicating the importance of patch drying. Concerning skin retention, the bioadhesive film produced a reduction of the amount of sumatriptan remaining in the skin, but this can be advantageous in the control of drug input, since it reduces the reservoir effect in the skin and allows for an immediate interruption of drug input when the patch is removed.
Femenía-Font
A
A
Departamento de Fisiología, Farmacología y Toxicología, Facultad de Ciencias Experimentales y de la Salud, Universidad Cardenal Herrera-CEU, 46113 Moncada, Spain.
Padula
C
C
Marra
F
F
Balaguer-Fernández
C
C
Merino
V
V
López-Castellano
A
A
Nicoli
S
S
Santi
P
P
D000279:Administration, Cutaneous; D000818:Animals; D016503:Drug Delivery Systems; D005026:Ethylene Glycols / Q000494:pharmacology*; D066298:In Vitro Techniques; D010539:Permeability / Q000187:drug effects; D011092:Polyethylene Glycols / Q000494:pharmacology*; D011760:Pyrrolidinones / Q000494:pharmacology; D011817:Rabbits; D012867:Skin / Q000187:drug effects / Q000378:metabolism; D012869:Skin Absorption / Q000187:drug effects*; D018170:Sumatriptan / Q000008:administration & dosage* / Q000493:pharmacokinetics; D014662:Vasoconstrictor Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics
D005026:Ethylene Glycols; D011760:Pyrrolidinones; D014662:Vasoconstrictor Agents; D011092:Polyethylene Glycols; D018170:Sumatriptan; C010111:carbitol; C028537:2-pyrrolidone