Crosslinked poly(methyl vinyl ether-co-maleic anhydride) as topical vehicles for hydrophilic and lipophilic drugs.
Poly(methyl vinyl ether-co-maleic anhydride) crosslinked with ethylene glycol (GZ-ET), 1,4-butanediol (GZ-BUT), 1,6-exandiol (GZ-EX), 1,8-octanediol (GZ-OCT), 1,10-decanediol (GZ-DEC) or 1,12-dodecanediol (GZ-DOD) was prepared and employed as a supporting material for aqueous topical gels containing pyridoxine hydrochloride (PYCL) chosen as a hydrophilic model molecule or for O/A emulsion containing beta-carotene chosen as a hydrophobic model molecule. We analyzed the effect of the nature of the crosslinker on the permeation of hydrophilic and lipophilic vitamins through porcine skin by in vitro permeation studies. The vehicles formed by crosslinked poly(methyl vinyl ether-co-maleic anhydride) showed enhanced vitamins permeation with respect to the same vehicles formed by noncrosslinked poly(methyl vinyl ether-co-maleic anhydride) (GZ). The decrease in the crosslinker acyl chain length provides vehicles accelerating the drug permeability through the skin.
Luppi
B
B
Department of Pharmaceutical Sciences, Bologna University, Bologna, Italy. bluppi@biocfarm.unibo.it
Cerchiara
T
T
Bigucci
F
F
Di Pietra
A M
AM
Orienti
I
I
Zecchi
V
V
D000287:Administration, Topical; D000818:Animals; D003432:Cross-Linking Reagents / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D004337:Drug Carriers / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D005782:Gels; D008055:Lipids / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D008298:Maleates / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D010539:Permeability / Q000187:drug effects; D011145:Polyvinyls / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D012867:Skin / Q000187:drug effects* / Q000378:metabolism; D013552:Swine; D019207:beta Carotene / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics
D003432:Cross-Linking Reagents; D004337:Drug Carriers; D005782:Gels; D008055:Lipids; D008298:Maleates; D011145:Polyvinyls; C058026:polyvinylmethoxyethylene-maleic anhydride copolymer; D019207:beta Carotene