6533b854fe1ef96bd12ae947
RESEARCH PRODUCT
In vitro evaluation of glycol chitosan based formulations as oral delivery systems for efflux pump inhibition.
Gaetano GiammonaMaria Grazia PerroneGiuseppe TrapaniNicola Antonio ColabufoDelia MandracchiaGiuseppe TripodoAdriana Trapanisubject
endocrine systemATP Binding Cassette Transporter Subfamily BPolymers and Plastics02 engineering and technologyPharmacologyDosage formChitosan03 medical and health scienceschemistry.chemical_compoundGlycols0302 clinical medicineDrug Delivery SystemsOral administrationhealth services administrationpolycyclic compoundsMaterials ChemistryHumansGlycol chitosan-based formulations P-gp inhibition properties Rhodamine 123 Glycol chitosan-4-thiobutylamidine thiomer Caco-2 cells Oral bioavailabilityChitosanChemistryThiomerOrganic ChemistryGlycol chitosan-based formulations P-gp inhibition properties Rhodamine 123 Glycol chitosan-4-thiobutylamidine thiomer Caco-2 cells Oral bioavailability021001 nanoscience & nanotechnologyBioavailabilityCaco-2Settore CHIM/09 - Farmaceutico Tecnologico Applicativo030220 oncology & carcinogenesisNanoparticlessense organsEffluxCaco-2 Cells0210 nano-technologyhormones hormone substitutes and hormone antagonistsConjugatedescription
Recently, we have reported that glycol chitosan (GCS) was able to reverse the P- glycoprotein (P-gp) efflux pump. The objective of the present study was to evaluate the potential of two GCS-based dosage forms (aqueous solution or nanoparticle suspension) for oral administration of the P-gp substrate Rho-123. A further aim of the present study was to assess the effect of the glycol chitosan-4-thiobutylamidine thiomer (GCS-TBA) on P-gp activity considering that the corresponding thiomer of chitosan series is a well-known P-gp inhibitor. Pre-treatment of Caco-2 cell monolayer with a GCS solution or GCS-based nanoparticles increased the absorptive transport of Rho-123 across the monolayer of 1.43-fold. The modification of GCS with 2-iminothiolane led to GCS-TBA conjugate which did not show any P-gp inhibitory activity. Therefore, GCS polymer and corresponding dosage forms may contribute to increase the oral bioavailability of Pgp-substrate drugs, while GCS-TBA cannot be used for the same purpose.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2017-01-01 | Carbohydrate polymers |