Influence of chitosan and polycarbophil on permeation of a model hydrophilic drug into the urinary bladder wall.
Influence of dispersions of mucoadhesive polymers chitosan and polycarbophil on permeability properties of urinary bladder was investigated in vitro on isolated porcine urinary bladder. Pipemidic acid as a model hydrophilic drug was used. Its distribution in the bladder wall was determined from actual tissue concentrations by a method based on sectioning of frozen tissue and extraction of tissue slices. Pipemidic acid tissue concentration versus tissue depth profiles were evaluated by a diffusion model assuming constant diffusion coefficient. Increase in bladder wall permeability was observed in the presence of both polymers. Apparent permeability (mean+/-S.D.) of urinary bladder wall was increased 2.7+/-2.9 and 2.8+/-2.0 times for chitosan, and 2.3+/-2.0 and 4.3+/-4.2 times for polycarbophil at 0.5 and 1.0%, w/v polymer concentration, respectively. This increase is a consequence of the increased permeability of urothelium. These findings support investigations on application of chitosan and polycarbophil in development of mucoadhesive intravesical drug delivery systems. Experimental model may be applied to evaluate the results of experiments with drugs used in intravesical therapy.
Grabnar
I
I
Faculty of Pharmacy, University of Ljubljana, Askerceva 7, 1000, Ljubljana, Slovenia. iztok.grabnar@ffa.uni-lj.si
Bogataj
M
M
Mrhar
A
A
D000180:Acrylic Resins / Q000494:pharmacology*; D000283:Administration, Intravesical; D000818:Animals; D000892:Anti-Infective Agents, Urinary / Q000493:pharmacokinetics*; D001692:Biological Transport / Q000187:drug effects; D002686:Chitin / Q000031:analogs & derivatives* / Q000494:pharmacology*; D048271:Chitosan; D002851:Chromatography, High Pressure Liquid; D004337:Drug Carriers / Q000494:pharmacology; D066298:In Vitro Techniques; D008954:Models, Biological; D010539:Permeability / Q000187:drug effects; D010876:Pipemidic Acid / Q000493:pharmacokinetics*; D013552:Swine; D001743:Urinary Bladder / Q000378:metabolism*; D019459:Urothelium / Q000166:cytology / Q000378:metabolism
D000180:Acrylic Resins; D000892:Anti-Infective Agents, Urinary; D004337:Drug Carriers; D002686:Chitin; C030312:calcium polycarbophil; D048271:Chitosan; D010876:Pipemidic Acid