In-vitro characterization of buccal iontophoresis: the case of sumatriptan succinate.
Buccal administration of sumatriptan succinate might be an interesting alternative to the present administration routes, due to its non-invasiveness and rapid onset of action, but because of its low permeability, a permeation enhancement strategy is required. The aim of this work was then to study, in-vitro, buccal iontophoresis of sumatriptan succinate. Permeation experiments were performed in-vitro across pig esophageal epithelium, a recently proposed model of human buccal mucosa, using vertical diffusion cells. The iontophoretic behavior of the tissue was characterized by measuring its isoelectric point (Na(+) transport number and the electroosmotic flow of acetaminophen determination) and by evaluating tissue integrity after current application. The results obtained confirm the usefulness of pig esophageal epithelium as an in-vitro model membrane for buccal drug delivery. The application of iontophoresis increased sumatriptan transport, proportionally to the current density applied, without tissue damage: electrotransport was the predominant mechanism. Integrating the results of the present work with literature data on the transport of other molecules across the buccal mucosa and across the skin, we can draw a general conclusion: the difference in passive transport across buccal mucosa and across the skin is influenced by permeant lipophilicity and by the penetration pathway. Finally, buccal iontophoretic administration of sumatriptan allows to administer 6mg of the drug in 1h, representing a promising alternative to the current administration routes.
Department of Pharmacy, University of Parma, Parco Area delle Scienze 27/a, 43124 Parma, Italy.
Isabella
I
Telò
Department of Pharmacy, University of Parma, Parco Area delle Scienze 27/a, 43124 Parma, Italy.
Elena
E
Tratta
Department of Pharmacy, University of Parma, Parco Area delle Scienze 27/a, 43124 Parma, Italy.
Barbara
B
Guasconi
Department of Pharmacy, University of Parma, Parco Area delle Scienze 27/a, 43124 Parma, Italy.
Sara
S
Nicoli
Department of Pharmacy, University of Parma, Parco Area delle Scienze 27/a, 43124 Parma, Italy.
Silvia
S
Pescina
Department of Biomedical, Biotechnological and Traslational Sciences, University of Parma, Via Gramsci 14, 43126 Parma, Italy.
Paolo
P
Govoni
Department of Pharmacy, University of Parma, Parco Area delle Scienze 27/a, 43124 Parma, Italy.
Patrizia
P
Santi
Department of Pharmacy, University of Parma, Parco Area delle Scienze 27/a, 43124 Parma, Italy. Electronic address: cristina.padula@unipr.it.
Cristina
C
Padula
D000082:Acetaminophen / Q000493:pharmacokinetics; D000278:Administration, Buccal; D000818:Animals; D001692:Biological Transport; D016503:Drug Delivery Systems; D007478:Iontophoresis; D007526:Isoelectric Point; D023421:Models, Animal; D009061:Mouth Mucosa / Q000378:metabolism*; D010539:Permeability; D058825:Serotonin 5-HT1 Receptor Agonists / Q000008:administration & dosage* / Q000493:pharmacokinetics; D012869:Skin Absorption; D018170:Sumatriptan / Q000008:administration & dosage* / Q000493:pharmacokinetics; D013552:Swine
D058825:Serotonin 5-HT1 Receptor Agonists; D000082:Acetaminophen; D018170:Sumatriptan
Acetaminophen (PubChem CID: 1983); Electroosmotic flow; Iontophoresis; Isoelectric point; Lidocaine hydrochloride; Lidocaine hydrochloride (PubChem CID: 6314); Permselectivity; Porcine esophageal epithelium; Sumatriptan succinate; Sumatriptan succinate (PubChem CID: 59772)