title: Transdermal and buccal delivery of methylxanthines through human tissue in vitro.
abstract: We examined the in vitro permeation of central nervous stimulants - caffeine, theophylline, and theobromine across human skin with the aid of six chemical enhancers. It was found that oleic acid was the most potent enhancer for all three methylxanthines. Further optimization studies with different solvents showed that caffeine transport could be enhanced to give flux values up to 585 microg/cm2.hr-1. Theobromine and theophylline delivery rates proved insufficient. An additional study involving a buccal tissue equivalent showed that this membrane was more permeable than skin for all model actives tested and would offer an alternate way of delivery.
authors.affiliation: Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, Piscataway, NJ 08854, USA.
authors.forename: Rashmi A
authors.initials: RA
authors.lastname: Thakur
authors.forename: Bozena B
authors.initials: BB
authors.lastname: Michniak
authors.forename: Victor M
authors.initials: VM
authors.lastname: Meidan
mesh_terms: D000278:Administration, Buccal; D000279:Administration, Cutaneous; D002110:Caffeine / Q000008:administration & dosage / Q000493:pharmacokinetics*; D000697:Central Nervous System Stimulants / Q000008:administration & dosage / Q000493:pharmacokinetics*; D005079:Excipients / Q000494:pharmacology*; D006801:Humans; D066298:In Vitro Techniques; D009061:Mouth Mucosa; D019301:Oleic Acid / Q000494:pharmacology; D010539:Permeability; D012867:Skin; D012869:Skin Absorption; D012995:Solubility; D013805:Theobromine / Q000008:administration & dosage / Q000493:pharmacokinetics*; D013806:Theophylline / Q000008:administration & dosage / Q000493:pharmacokinetics*; D014966:Xanthenes / Q000008:administration & dosage / Q000493:pharmacokinetics*
chemical_list: D000697:Central Nervous System Stimulants; D005079:Excipients; D014966:Xanthenes; D019301:Oleic Acid; D002110:Caffeine; D013806:Theophylline; D013805:Theobromine