The present study aimed at exploring the potential of the P-glycoprotein (P-gp) transporters as a barrier to the repaglinide (REG) epithelial permeability. In-vitro intestinal absorption models, the everted gut sac, and Caco-2 cell line, were used to study the possible role of P-gp in intestinal transport of REG. In the everted gut sacs, apparent permeability coefficients showed cargo concentra...

The present study aimed at exploring the potential of the P-glycoprotein (P-gp) transporters as a barrier to the repaglinide (REG) epithelial permeability. In-vitro intestinal absorption models, the everted gut sac, and Caco-2 cell line, were used to study the possible role of P-gp in intestinal transport of REG. In the everted gut sacs, apparent permeability coefficients showed cargo concentra...

The objective of this study was to investigate the influence of physiochemical parameters (such as size, molecular weight, molecular geometry, and number of surface amine groups) of poly (amidoamine) (PAMAM) dendrimers, on their permeability across Caco-2 cell monolayers. The permeability of a series of PAMAM dendrimers, generations 0-4 (G0-G4), was investigated across Caco-2 cell monolayers in...

background and objectives: in the original in vitro method for evaluation of iron bioavailability using caco-2 cell model, ferritin formation by cells is considered as a functional indicator of both absorption and utilization of iron. however, as iron is measured in the tested material and then ferritin concentration is measured in caco-2 cell lysate, it is almost impossible to have a concrete ...

A series of arylketo-containing P1-P3 linked macrocyclic BACE-1 inhibitors were designed, synthesized, and compared with compounds with a previously known and extensively studied corresponding P2 isophthalamide moiety with the aim to improve on permeability whilst retaining the enzyme- and cell-based activities. Several inhibitors displayed substantial increases in Caco-2 cell-based permeabilit...

The intestinal permeability of low-molecular-weight hyaluronan (LMW-HA) was investigated by using cultured monolayers of Caco-2 cells. The amount of LMW-HA that permeated the Caco-2 monolayers was measured by a carbazole assay. The permeability of LMW-HA increased inversely with the molecular size and was dose-dependent. The transport was observed to be energy-independent, and was correlated wi...

The intestinal absorption of chondroitin sulfate (CS) and its hydrolysate, particularly the disaccharides (Di-CS), was investigated by using human intestinal epithelial Caco-2 cell monolayers. Although the transepithelial transport of CS was not detectable, dose- and time-dependent transport of Di-CS was observed. The transport of Di-CS was proved to be energy-independent and its permeability i...

Cell lines are the invitro models used for the drug permeability studies in the preclinical and clinical phases of the drug discovery. Cell line models are simple and quick to use and avoids the usage of animal models for pharmacological and toxicological studies and hence cost effective, produce reliable and reproducible results for understanding and evaluating the permeability characteristics...

Several in vitro assays have been developed to evaluate the gastrointestinal absorption of compounds. Our aim was to compare 3 of these methods: 1) the bio-mimetic artificial membrane permeability assay (BAMPA) method, which offers a high-throughput, noncellular approach to the measurement of passive transport; 2) the traditional Caco-2 cell assay, the use of which as a high-throughput tool is ...