Chitosan-N-acetyl cysteine conjugates: in vitro evaluation of permeation enhancing and P-glycoprotein inhibiting properties.
This study evaluated three chitosan-N-acetyl cysteine (CAC) conjugates of increasing molecular mass as a valuable tool to improve the absorption of drugs by assessing its permeation enhancing effect regarding the active P-gp substrate rhodamine-123 in comparison to the trans- and paracellular marker FD 4 both in rat intestine and Caco 2 monolayers. Additional LDH and MTT cytotoxicity tests have attested a non-toxic profile to CAC, which can consequently be seen as a safe and promising novel drug carrier with the ability to enhance drug absorption and to inhibit P-gp efflux transporters.
Schmitz
Thierry
T
Institute of Pharmacy, Department of Pharmaceutical Technology, University of Innsbruck, Innsbruck, Austria.
Hombach
Juliane
J
Bernkop-Schnürch
Andreas
A
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000037:antagonists & inhibitors*; D000111:Acetylcysteine / Q000737:chemistry* / Q000494:pharmacology; D000818:Animals; D018938:Caco-2 Cells; D048271:Chitosan / Q000737:chemistry* / Q000494:pharmacology; D003911:Dextrans / Q000493:pharmacokinetics; D004337:Drug Carriers / Q000737:chemistry; D005452:Fluoresceins / Q000493:pharmacokinetics; D006801:Humans; D066298:In Vitro Techniques; D007770:L-Lactate Dehydrogenase / Q000378:metabolism; D008970:Molecular Weight; D010539:Permeability / Q000187:drug effects; D051381:Rats; D020112:Rhodamine 123 / Q000493:pharmacokinetics; D018675:Toxicity Tests
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D003911:Dextrans; D004337:Drug Carriers; D005452:Fluoresceins; C052526:fluorescein-dextran; D020112:Rhodamine 123; D048271:Chitosan; D007770:L-Lactate Dehydrogenase; D000111:Acetylcysteine