title: Influence of formulation variables in transdermal drug delivery system containing zolmitriptan.
abstract: The effects of different formulation variables including pressure sensitive adhesive (PSA), thickness of the matrix, solvent system, inclusion of crystallization inhibitor, loading amount of drug and enhancers on the transdermal absorption of zolmitriptan were investigated. Acrylic adhesive with hydroxyl functional group provided good adhesion force and high flux of zolmitriptan. Pseudopolymorphs of zolmitriptan were found to possess different solid-state properties that affected the permeation rate. Polyoxyethylene alkyl ethers significantly increased the permeation of zolmitriptan through hairless mouse skin. However, these enhancers induced crystallization of zolmitriptan. Kollidon(®) 30 delayed the crystallization without altering the permeation profile of zolmitriptan. Stability studies suggested that terpenes did not induce crystallization of zolmitriptan in the patch and stable formulations could be produced by using cineole and limonene, or their combination.
authors.affiliation: BK21 Project Team, College of Pharmacy, Chosun University, 375 Seosuk-dong, Dong-gu, Gwangju 501-759, South Korea.
authors.forename: Robhash Kusam
authors.initials: RK
authors.lastname: Subedi
authors.forename: Je-Phil
authors.initials: JP
authors.lastname: Ryoo
authors.forename: Cheol
authors.initials: C
authors.lastname: Moon
authors.forename: Hoo-Kyun
authors.initials: HK
authors.lastname: Choi
mesh_terms: D000269:Adhesives / Q000737:chemistry; D000279:Administration, Cutaneous; D000818:Animals; D003460:Crystallization; D003511:Cyclohexanols / Q000737:chemistry; D053138:Cyclohexenes / Q000737:chemistry; D016503:Drug Delivery Systems; D000077591:Eucalyptol; D005079:Excipients / Q000737:chemistry*; D000077222:Limonene; D051379:Mice; D008812:Mice, Hairless; D039821:Monoterpenes / Q000737:chemistry; D023303:Oxazolidinones / Q000008:administration & dosage* / Q000493:pharmacokinetics; D010539:Permeability; D011092:Polyethylene Glycols / Q000737:chemistry; D011205:Povidone / Q000737:chemistry; D058825:Serotonin 5-HT1 Receptor Agonists / Q000008:administration & dosage* / Q000493:pharmacokinetics; D012869:Skin Absorption; D012997:Solvents / Q000737:chemistry; D013729:Terpenes / Q000737:chemistry; D057968:Transdermal Patch; D014363:Tryptamines / Q000008:administration & dosage* / Q000493:pharmacokinetics
chemical_list: D000269:Adhesives; D003511:Cyclohexanols; D053138:Cyclohexenes; D005079:Excipients; D039821:Monoterpenes; D023303:Oxazolidinones; C495681:Sanonic SS-90; D058825:Serotonin 5-HT1 Receptor Agonists; D012997:Solvents; D013729:Terpenes; D014363:Tryptamines; C089750:zolmitriptan; D011092:Polyethylene Glycols; D000077222:Limonene; D011205:Povidone; D000077591:Eucalyptol