Drug release from poly(acrylic acid) grafted poly(vinylidene fluoride) membrane bags in the gastrointestinal tract in the rat and dog.
Stomach-specific drug delivery systems would be of value in treating diseases of the upper gastrointestinal tract. The present study measured in vitro and in vivo drug release from pH-sensitive membrane bags, constructed of poly(acrylic acid) grafted onto a poly(vinylidene fluoride) (PAA-PVDF) membrane, which might be suitable for stomach-specific drug delivery. The used model drugs were propranolol-HCl (1.0 mg) and FITC-dextran MW 4400 (1.0 mg). Drug release in vivo was studied by inserting membrane bags into the stomach and proximal duodenum of anesthetized rats and dogs. At 30 and 180 min, the bags were removed from the lumens and residual drug content was determined. The release of either propranolol or FITC-dextran were comparable in both stomach and duodenum, showing that in vivo drug release did not depend on environmental pH. In vitro results suggested that these results could be explained by interactions between PAA and the mucous layers of the stomach and duodenum.
Tarvainen
T
T
Department of Pharmaceutics, University of Kuopio, PO Box 1627, 70211, Kuopio, Finland. tommy.tarvainen@uku.fi
Nevalainen
T
T
Sundell
A
A
Svarfvar
B
B
Hyrsylä
J
J
Paronen
P
P
Järvinen
K
K
D000180:Acrylic Resins / Q000737:chemistry*; D000319:Adrenergic beta-Antagonists / Q000008:administration & dosage / Q000493:pharmacokinetics; D000818:Animals; D003911:Dextrans; D004064:Digestive System / Q000378:metabolism*; D004285:Dogs; D016503:Drug Delivery Systems; D004386:Duodenum / Q000378:metabolism; D016650:Fluorescein-5-isothiocyanate / Q000031:analogs & derivatives; D006863:Hydrogen-Ion Concentration; D008297:Male; D008567:Membranes, Artificial; D011145:Polyvinyls / Q000737:chemistry*; D011433:Propranolol / Q000008:administration & dosage / Q000493:pharmacokinetics; D051381:Rats; D017208:Rats, Wistar; D005465:Fluorocarbon Polymers
D000180:Acrylic Resins; D000319:Adrenergic beta-Antagonists; D003911:Dextrans; D016650:Fluorescein-5-isothiocyanate; D008567:Membranes, Artificial; D011145:Polyvinyls; D011433:Propranolol; C015219:fluorescein isothiocyanate dextran; C024865:polyvinylidene fluoride; D005465:Fluorocarbon Polymers; C006903:carbopol 940