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N-(2-hydroxypropyl)methacrylamide (HPMA)-based copolymers have been shown to be efficient carriers for anticancer drugs because of their versatile chemistry and good biocompatibility. As demonstrated with hepatocytes, targeting efficacy of anticancer drugs could be further improved when the drug (doxorubicin) was conjugated to HPMA copolymers with(More)
A series of boronated cationic copolymers, composed of different ratios of acrylamide, N-acryloyl-3-aminophenylboronic acid and N-acryloyl-diaminoethane (the cationic moiety), were prepared with the intention of localizing boron neutron capture therapy (BNCT) in experimentally induced polyps on the luminal side of the gut of the rat. The goals of this study(More)
N-(2-hydroxypropyl)methacrylamide (HPMA) copolymers containing pendant saccharide moieties (galactosamine, lactose, and triantennary galactose) were synthesized. The relationship between the content of saccharide moieties and three-dimensional arrangement of galactose residues and their biorecognition and internalization by human hepatocarcinoma HepG2 cells(More)
Calcium pectinate (CaP)—the insoluble salt of pectin—can potentially be used as a colon-specific drug delivery system. The use of CaP as a carrier was based on the assumption that, like pectin, it can be decomposed by specific pectinolytic enzymes in the colon but that it retains its integrity in the physiological environment of the small bowel. The(More)
The ability of the gastrointestinal (GI) tract, as well as other tissues, to cope with reactive oxygen species (ROS) efflux in pathological events is determined partly by epithelial antioxidant levels. These levels are comprized of tissue antioxidant enzymes and low molecular weight antioxidants (LMWA). While glutathione levels and the activity of enzymatic(More)
The human gastrointestinal tract consists of a highly complex ecosystem of aerobic and anaerobic microorganisms that plays a significant role in the metabolism of nutrients as well as drugs. In the colon, bacteria ferment various types of substrates that are not susceptible to digestion in the small intestine. This arouses interest in specific drugs, drug(More)
  • A Rubinstein
  • 1995
With the determination of the exact mode of action of sulfasalazine 20 years ago, attention and interest was drawn to the colonic delivery of drugs. A few years before that it became clear that some orally administered laxative drugs are active only after arrival at the large intestine. This resulted in research activity that led to the development of(More)
The thickness of the mucus gel and its turnover rate were measured in the stomach, proximal jejunum, cecum and proximal colon of the rat, using microscopy and staining techniques. The specific mucus-secretory responses to carbachol-induced cholinergic stimulus in these locations were also studied. The mucus gel was found to be the thinnest (18 ±1 microns)(More)
The successful functioning of oral medication depends primarily on how the gastrointestinal (Gl) tract processes drugs and drug delivery systems. Parameters such as regional pH, motility (and hence residence time), and brush border and colonic microflora enzymatic activity play an important role in the performance of orally administered dosage forms. In(More)