Search results for "Caco-2"
showing 10 items of 203 documents
Impact of uncharged and charged stabilizers on in vitro drug performances of clarithromycin nanocrystals
2018
The purpose of this study was to evaluate the effect of charge on the in vitro drug performances of clarithromycin nanocrystals. To prepare different charges of nanocrystals, media milling was employed with the use of different stabilizing systems. The uncharged nanocrystals were prepared from poloxamer 407. The negatively and positively charged nanocrystals were stabilized using a combination of poloxamer 407 with sodium lauryl sulfate (SLS) and cetyltrimethylammonium bromide (CTAB), respectively. After production, the particle size of the negatively and positively charged nanocrystals was smaller than that of the uncharged one. The similar particle size of variously charged clarithromycin…
Availability of polyphenols in fruit beverages subjected to in vitro gastrointestinal digestion and their effects on proliferation, cell-cycle and ap…
2009
Abstract Three fruit beverages: Fb (grape–orange–apricot), FbFe (Fb + iron sulphate) and FbFeM (FbFe + skimmed milk) were subjected to in vitro gastrointestinal digestion. Addition of Fe and milk decreased the phenolic content of Fb by 13% and 55%, respectively. The digestion process decreased the phenolic content by 47%, 60%, and 70% in Fb, FbFe and FbFeM with respect to the initial, non-digested, Fb. Caco-2 cells were incubated for 4 h daily for four days or continuously for 24 h with bioaccessible fractions obtained after the digestion (digests). Polyphenols were not metabolised by Caco-2 cells. Fb digest (∼50 μM total phenolics) was the sample that led to the highest inhibition of cell …
Interaction effects of enniatin B, deoxinivalenol and alternariol in Caco-2 cells.
2015
Enniatin B (ENN B), deoxinivalenol (DON) and alternariol (AOH) are secondary metabolites of filamentous fungi. These mycotoxins are contaminants of vegetables and cereals. They are cytotoxic and their effects are enhanced by their mixtures. The objectives of this study were to compare the cytotoxicity of ENN B, DON and AOH alone or in combination in human adenocarcinoma (Caco-2) cells and to evaluate the type of interactions of mycotoxin mixtures by the isobologram analysis. Cells were treated with concentrations ranging from 1.85 to 90μM (AOH) and from 0.312 to 10μM (for ENN B and DON), individually and in combination of two and three mycotoxins (from 1.85 to 30μM for AOH and from 0.312 to…
Amphiphilic poly(hydroxyethylaspartamide) derivative-based micelles as drug delivery systems for ferulic acid
2008
Self-assembling micelles, potentially useful as drug delivery systems for ferulic acid (FA), were obtained in aqueous media from amphiphilic alpha,beta-poly(N-2-hydroxyethyl)-dl-aspartamide (PHEA) copolymers bearing at the polyamino acidic backbone both poly(ethyleneglycol) (2000 or 5000 Da) and hexadecylamine (C(16)) moieties, at a concentration of 7 x 10(- 3) and 4 x 10(- 3) g/l, respectively, with nanometre size and negative zeta potential. These micelles were able to entrap FA and to release it in a prolonged way in phosphate buffer solution at pH 7.4 and human plasma. These systems were also stable in storage conditions and have no cytotoxic effects on Caco-2, 16 HBE, HuDe and K562 cel…
Heme oxygenase-1 inhibits apoptosis in Caco-2 cells via activation of Akt pathway
2005
Heme oxygenase-1 can play a protective role against cellular stress. In colon cancer cells, these effects would be relevant to oncogenesis and resistance to chemotherapy. The aim of the study was to examine the effects of heme oxygenase-1 induction on cell survival in a human colon cancer cell line, Caco-2. Serum deprivation induced apoptosis, reduced Akt and p38 phosphorylation, and increased p21(Cip/WAF1) levels. Heme oxygenase-1 induction by treatment with cobalt protoporphyrin IX resulted in resistance to apoptosis, activation of Akt, reduction in p21(Cip/WAF1) levels and modification of bcl2/bax ratio towards survival. Indomethacin reduced apoptosis but in contrast to heme oxygenase-1,…
Advanced strategy to exploit wine-making waste by manufacturing antioxidant and prebiotic fibre-enriched vesicles for intestinal health.
2020
Grape extract-loaded fibre-enriched vesicles, nutriosomes, were prepared by combining antioxidant extracts obtained from grape pomaces and a prebiotic, soluble fibre (Nutriose®FM06). The nutriosomes were small in size (from ∼140 to 260 nm), homogeneous (polydispersity index < 0.2) and highly negative (∼ −79 mV). The vesicles were highly stable during 12 months of storage at 25 °C. When diluted with warmed (37 °C) acidic medium (pH 1.2) of high ionic strength, the vesicles only displayed an increase of the mean diameter and a low release of the extract, which were dependent on Nutriose concentration. The formulations were highly biocompatible and able to protect intestinal cells (Caco-2) fro…
Induction of Human P-Glycoprotein in Caco-2 cells: Development of a Highly Sensitive Assay System for P-Glycoprotein-Mediated Drug Transport
2006
The aim of this work is to develop a highly sensitive assay system for P-gp-mediated transport by using two methods, induction of P-gp and short-term culture of Caco-2 cells. To induce P-gp in Caco-2 cells, cells were cultured in vinblastine-containing medium. The mRNA level of P-gp was approximately 7-fold higher in Caco-2 cells cultured with vinblastine (P-gp-induced Caco-2 cells) than in control cells. Western blot analysis showed a significant increase in P-gp expression. After cell differentiation, the mRNA level of P-gp was downregulated, however, P-gp-induced Caco-2 cells still possessed a 5.6-fold higher mRNA level of P-gp compared to control cells. Polarized transport of substrate …
Studies on a new potential dopaminergic agent: in vitro BBB permeability, in vivo behavioural effects and molecular docking evaluation.
2015
2-Amino-N-[2-(3,4-dihydroxy-phenyl)-ethyl]-3-phenyl-propionamide (DA-PHEN) has been previously synthesized to obtain a potential prodrug capable of release dopamine (DA) into CNS. However, DA-PHEN could act per se as a dopaminergic drug. In this study, the permeability transport (Pe), obtained by parallel artificial permeability assay (PAMPA), indicated a low passive transcellular transport (Pe = 0.32 ± 0.01 × 10(-6 )cm/s). Using the Caco-2 cell system, the Papp AP-BL in absorptive direction (3.36 ± 0.02 × 10(-5 )cm/s) was significantly higher than the Papp BL-AP in secretive direction (1.75 ± 0.07 × 10(-5 )cm/s), suggesting a polarized transport. The efflux ratio (Papp AP-BL/Papp BL-AP = 0…
Biowaiver monographs for immediate-release solid oral dosage forms: Zidovudine (azidothymidine).
2012
Literature data on the properties of zidovudine relevant to waiver of in vivo bioequivalence (BE) testing requirements for the approval of immediate-release (IR) solid oral dosage forms containing zidovudine alone or in combination with other active pharmaceutical ingredients (APIs) are reviewed. Solubility, dissolution, and permeability data for zidovudine, along with its dosing schedule, therapeutic index and pharmacokinetic properties, and reports related to BE/bioavailability were all taken into consideration. Data for solubility and permeability suggest that zidovudine belongs to Class I according to the Biopharmaceutics Classification System. Also, zidovudine is not a narrow therapeut…
Provisional Classification and in Silico Study of Biopharmaceutical System Based on Caco-2 Cell Permeability and Dose Number
2013
Today, early characterization of drug properties by the Biopharmaceutics Classification System (BCS) has attracted significant attention in pharmaceutical discovery and development. In this direction, the present report provides a systematic study of the development of a BCS-based provisional classification (PBC) for a set of 322 oral drugs. This classification, based on the revised aqueous solubility and the apparent permeability across Caco-2 cell monolayers, displays a high correlation (overall 76%) with the provisional BCS classification published by World Health Organization (WHO). Current database contains 91 (28.3%) PBC class I drugs, 76 (23.6%) class II drugs, 97 (31.1%) class III d…