Search results for "Caco-2 cell"
showing 10 items of 170 documents
Predictive Toxicology of Cobalt Nanoparticles and Ions: Comparative In Vitro Study of Different Cellular Models Using Methods of Knowledge Discovery …
2011
The toxicological effects of cobalt nanoparticles (Co-NPs) aggregates were examined and compared with those of cobalt ions (Co-ions) using six different cell lines representing lung, liver, kidney, intestine, and the immune system. Dose-response curves were studied in the concentration range of 0.05-1.0 mM, employing 3-(4,5-dimethylthiazol-2-Yl)-2,5-diphenyltetrazolium bromide test, neutral red, and Alamar blue as end point assays following exposures for 48 and 72 h. Data analysis and predictive modeling of the obtained data sets were executed by employing a decision tree model (J48), where training and validation were carried out by an iterative process. It was established, as expected, th…
Caki-1 Cells Represent an in vitro Model System for Studying the Human Proximal Tubule Epithelium
2007
<i>Background/Aims:</i> The human proximal tubule (PT) epithelium is distinguished from other nephron segments via several unique characteristics. Studies assessing PT epithelium increasingly employ cell lines, bypassing the complexity of primary cell cultures. However, few human model systems exist for studying PT cells in vitro. The current work involves an intensive characterization of Caki-1 cells, a commercially available human renal cell line. <i>Methods:</i> Caki-1 cells were validated as a representative model system for PT cell research via morphological, physiological and biochemical investigations including light and transmission electron microscopy, trans…
Biowaiver Monographs for Immediate-Release Solid Oral Dosage Forms: Folic Acid.
2018
This work presents a review of literature and experimental data relevant to the possibility of waiving pharmacokinetic bioequivalence studies in human volunteers for approval of immediate-release solid oral pharmaceutical forms containing folic acid as the single active pharmaceutical ingredient. For dosage forms containing 5 mg folic acid, the highest dose strength on the World Health Organization Essential Medicines List, the dose/solubility ratio calculated from solubility studies was higher than 250 mL, corresponding to a classification as "not highly soluble." Small, physiological doses of folic acid (≤320 μg) seem to be absorbed completely via active transport, but permeability data f…
Resveratrol mediated cancer cell apoptosis, and modulation of multidrug resistance proteins and metabolic enzymes.
2019
Abstract Background The degree of intracellular drug accumulation by specific membrane transporters, i.e., MDR1, BCRP, and MRP, and the degree of detoxification by intracellular metabolic enzymes, i.e., CYP3A4 and GST, provide control for cancer chemotherapy through diminishing the propensity of cancer cells to undergo apoptosis which in turn modulates the unresolved and complex phenomenon of multidrug resistance (MDR) for the cancer cells. Hypothesis/Purpose This study dwells into the interaction details involving ABC-transporters, CYP3A4, GST and cytotoxic effects of resveratrol on different cell lines. Methods Resveratrol was evaluated for its ability modulating the expression and efflux…
Poly(alkylidenimine) Dendrimers Functionalized with the Organometallic Moiety [Ru(η5-C5H5)(PPh3)2]+ as Promising Drugs Against Cisplatin-Resistant Ca…
2018
Here and for the first time, we show that the organometallic compound [Ru(&eta
Variability of permeability estimation from different protocols of subculture and transport experiments in cell monolayers.
2014
Abstract Introduction In vitro models with high predictive ability have been revealed as strong tools for pharmaceutical industry. However, the variability in permeability estimations complicates the comparison and combination of data from different laboratories and it makes necessary the careful validation of the model and the continuous suitability demonstration. The adequate standardization of pre-experimental, experimental and post-experimental factors might help to reduce the inter- and intra-laboratory variability in permeability values. Methods The objective of this paper is the evaluation of the effect of passage number, experimental protocol, time after seeding and calculation meth…
Calcium, iron and zinc uptakes by Caco-2 cells from white beans and effect of cooking
2006
White beans (Phaseolus vulgaris L.) have an interesting content of essential elements, calcium, iron and zinc, but they content also phytates, oxalates, proteins, polyyphenols and complex polysaccharides that are known to interact with minerals and to affect their bioavailability. The bioavailability of calcium, iron and zinc from raw and cooked white beans was estimated using their uptake by Caco-2 cells as the criteria. Previously, the mineral fraction (soluble or dialysable) to be added to the Caco-2 cell monolayer was selected. The results obtained show that cooking increases the Caco-2 cells' uptake percentages (calcium, 18.8 versus 3.6; iron, 33.7 versus 1.7; and zinc, 17.2 versus 2.1…
Biodegradable and pH-sensitive hydrogels for potential colon-specific drug delivery: Characterization and in vitro release studies
2008
A novel pH-sensitive and biodegradable composite hydrogel, based on a methacrylated and succinic derivative of dextran, named Dex-MA-SA, and a methacrylated and succinic derivative of alpha,beta-poly( N-2-hydroxyethyl)- DL-aspartamide (PHEA), named PHM-SA, was produced by photocross-linking. The goal was to obtain a colon-specific drug delivery system, exploiting both the pH-sensitive behavior and the colon-specific degradability. The hydrogel prepared with a suitable ratio between the polysaccharide and the polyaminoacid was characterized regarding its swelling behavior in gastrointestinal simulated conditions, chemical and enzymatic degradability, interaction with mucin, and cell compatib…
Partially Quarternized Amino Functional Poly(methacrylate) Terpolymers: Versatile Drug Permeability Modifiers
2011
Partially quarternized poly(methacrylate) terpolymers (Q-BBMCs) have been synthesized, based on the basic butylated methacrylate copolymer (BBMC/EUDRAGIT E), an excipient approved by the Food and Drug Administration (FDA) and to date mainly applied for tablet coatings. Via straightforward polymer modification reactions, a series of Q-BBMCs with quarternization degrees of 22%, 42%, and 65% has been prepared. Apical to basolateral transport across Caco-2 cell monolayers was investigated, employing the paracellular transported compounds trospium and mannitol. At pH 6.5 quarternization resulted in increased permeation enhancement up to 2.8-fold compared to BBMC, that is, up to 7.3-fold compared…
in vitro biological evaluation of folate-functionalized block copolymer micelles for selective anti-cancer drug delivery.
2008
The main objective of this study was to evaluate the ability of folic acid-functionalized diblock copolymer micelles to improve the delivery and uptake of two poorly water-soluble anti-tumor drugs, tamoxifen and paclitaxel, to cancer cells through folate receptor targeting. The diblock copolymer used in this study comprised a hydrophilic poly[2-(methacryloyloxy)ethyl phosphorylcholine] (MPC) block, carrying at the chain end the folate targeting moiety, and a pH-sensitive hydrophobic poly[2-(diisopropylamino)ethyl methacrylate] (DPA) block (FA-MPC-DPA). The drug-loading capacities of tamoxifen- and paclitaxel-loaded micelles were determined by high performance liquid chromatography and the m…