A5058524919- Drug Transport and Resistance Mechanisms
- Drug Solubulity and Delivery Systems
- Pharmacological Effects and Toxicity Studies
- Advanced biosensing and bioanalysis techniques
- Antibiotics Pharmacokinetics and Efficacy
- Cancer Treatment and Pharmacology
- Crop Yield and Soil Fertility
- Advanced Drug Delivery Systems
- DNA and Nucleic Acid Chemistry
- Canadian Identity and History
- DNA and Biological Computing
- Nanoparticle-Based Drug Delivery
- RNA Interference and Gene Delivery
- Pediatric Hepatobiliary Diseases and Treatments
University of Southern Denmark
2019-2024
Swedish Chemicals Agency
2019
The oral bioavailability of paclitaxel is limited due to low solubility and high affinity for the P-glycoprotein (P-gp) efflux transporter. Here we hypothesized that maximizing intestinal levels through apparent enhancement controlling simultaneous release both P-gp inhibitor encequidar from amorphous solid dispersions (ASDs) would increase paclitaxel. ASDs in polyvinylpyrrolidone K30 (PVP-K30), hydroxypropylmethylcellulose 5 (HPMC-5), 4 K (HPMC-4K) were hence prepared by freeze-drying. In...
P-glycoprotein (P-gp) inhibitors, like zosuquidar, partly increase oral bioavailability of P-gp substrates, such as etoposide. Here, it was hypothesised that co-release etoposide and zosuquidar from amorphous solid dispersions (ASDs) may further bioavailability. This envisioned through simultaneous subsequent spatiotemporal association in the small intestinal lumen. To achieve this, ASDs polyvinylpyrrolidone (PVP), hydroxypropylmethyl cellulose (HPMC) 5, HPMC 4 k were prepared by...
Nucleotides that contain two nucleobases (double-headed nucleotides) have the potential to condense information of separate nucleotides into one. This presupposes both bases must successfully pair with a cognate strand. Here, double-headed feature cytosine, guanine, thymine, adenine, hypoxanthine, and diaminopurine linked C2'-position an arabinose scaffold were developed examined in full detail. These monomeric units efficiently prepared by convergent synthesis incorporated DNA...
P-glycoprotein inhibitors, like zosuquidar, have widely been used to study the role of in oral absorption. Still, systematic studies on inhibitor dose-response relationship intestinal drug permeation are lacking. In present study, we investigated effect 0.79 nM-2.5 μM zosuquidar etoposide permeability across Caco-2 cell monolayers. We also pharmacokinetics after or IV administration Sprague Dawley rats with co-administration 0.063–63 mg/kg as well itself. Oral bioavailability was 2.6–4.2%,...
P-glycoprotein (P-gp) limits the oral absorption of drug substances. Potent small molecule P-gp inhibitors (e.g., zosuquidar) and nonionic surfactants polysorbate 20) inhibit by proposedly different mechanisms. Therefore, it was hypothesised that a combination zosuquidar 20 may potentiate inhibition P-gp-mediated efflux. in assessed calcein-AM assay transcellular etoposide permeability study MDCKII-MDR1 Caco-2 cells. Furthermore, solutions etoposide, zosuquidar, were orally administered to...