Roles of acid/base nature and molecular weight in drug release from matrices of gelfoam and monoisopropyl ester of poly(vinyl methyl ether-maleic anhydride).
Ophthalmic drug inserts are usually placed in the conjunctival sac. Being in contact with the conjunctiva, they may provide means to deliver large and hydrophilic molecules, such as peptides and oligonucleotides into the eye. We evaluated Gelfoam and monoisopropyl ester of poly(vinyl methyl ether/maleic anhydride) (PVM/MA) as potential polymers for ocular inserts. Matrices were solvent cast with model drugs that had different pKa, molecular weight and hydrophilicity. Drug release from the matrices as well as charge and swelling of Gelfoam(R)-matrix were studied. The release of drugs from PVM/MA-matrices was by erosion of the polymer matrix. The molecular weight and other variants of the releasing compound did not affect their release. In Gelfoam(R)-matrices the release was diffusion controlled and it was affected by the pH of the external solution as well as the charge and molecular weight of the studied compound.
Hämäläinen
K M
KM
University of Kuopio, Department of Pharmaceutics, P.O.Box 1627, FIN-70211 Kuopio, Finland.
Määttä
E
E
Piirainen
H
H
Marianne Sarkola
Väisänen
A
A
Ranta
V P
VP
Urtti
A
A
D002021:Buffers; D003228:Conjunctiva; D003692:Delayed-Action Preparations; D003911:Dextrans / Q000008:administration & dosage / Q000737:chemistry; D004952:Esters / Q000008:administration & dosage / Q000737:chemistry; D016650:Fluorescein-5-isothiocyanate / Q000008:administration & dosage / Q000031:analogs & derivatives / Q000737:chemistry; D005452:Fluoresceins / Q000008:administration & dosage / Q000737:chemistry; D005665:Furosemide / Q000008:administration & dosage / Q000737:chemistry; D005781:Gelatin Sponge, Absorbable / Q000008:administration & dosage* / Q000737:chemistry*; D006863:Hydrogen-Ion Concentration; D008298:Maleates / Q000008:administration & dosage* / Q000737:chemistry*; D008353:Mannitol / Q000008:administration & dosage / Q000737:chemistry; D008970:Molecular Weight; D009883:Ophthalmic Solutions; D011095:Polyethylenes / Q000008:administration & dosage* / Q000737:chemistry*; D012590:Sclera; D013999:Timolol / Q000008:administration & dosage / Q000737:chemistry
D002021:Buffers; D003692:Delayed-Action Preparations; D003911:Dextrans; D004952:Esters; D005452:Fluoresceins; D008298:Maleates; D009883:Ophthalmic Solutions; D011095:Polyethylenes; C015219:fluorescein isothiocyanate dextran; C024098:6-carboxyfluorescein; D008353:Mannitol; D005665:Furosemide; D013999:Timolol; C043105:poly(methyl vinyl ether-co-maleic anhydride); D016650:Fluorescein-5-isothiocyanate