Sökning: "intracellular drug bioavailability"

Hittade 5 avhandlingar innehållade orden intracellular drug bioavailability.

  1. 1. Intracellular unbound drug concentrations : Methodology and application for understanding cellular drug exposure

    Författare :André Mateus; Per Artursson; Pär Matsson; José A. G. Morais; Jeff Krise; Uppsala universitet; []
    Nyckelord :MEDICAL AND HEALTH SCIENCES; MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; MEDICIN OCH HÄLSOVETENSKAP; MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; intracellular unbound drug concentrations; free drug; drug binding; drug transport; drug accumulation; cellular drug response; drug target engagement; Pharmaceutical Science; Farmaceutisk vetenskap;

    Sammanfattning : Most known drug targets and metabolizing enzymes are located inside cells. Interactions with these proteins are determined by intracellular unbound drug concentrations. Assessing intracellular drug exposure is technically challenging, but essential for predicting pharmacokinetic, pharmacological, and toxicological profiles of new drugs. LÄS MER

  2. 2. Characterization of parameters influencing intracellular bioavailability and prediction of intracellular drug exposure

    Författare :Andrea Treyer; Per Artursson; Gert Fricker; Uppsala universitet; []
    Nyckelord :MEDICAL AND HEALTH SCIENCES; MEDICIN OCH HÄLSOVETENSKAP; MEDICIN OCH HÄLSOVETENSKAP; MEDICAL AND HEALTH SCIENCES; intracellular drug bioavailability; unbound drug concentration; drug disposition; ADME; drug transport; drug metabolism membrane partitioning; phospholipid; drug-drug interaction; antisense oligonucleotide; cell-penetrating peptide; Farmaceutisk vetenskap; Pharmaceutical Science;

    Sammanfattning : This thesis work investigates factors influencing intracellular drug disposition. An experimental method for measurement of intracellular bioavailability (Fic), was used throughout. Fic is defined as the ratio between the unbound drug concentration inside the cell and the compound concentration in the cell exterior. LÄS MER

  3. 3. Dissolving the Rocks : Solubility Enhancement of Active Pharmaceutical Ingredients using Mesoporous Silica

    Författare :Xin Xia; Alfonso E. Garcia-Bennett; Xiaodong Zou; Göran Frenning; Stockholms universitet; []
    Nyckelord :NATURAL SCIENCES; NATURVETENSKAP; NATURVETENSKAP; NATURAL SCIENCES; mesoporous silica; drug delivery; solubility enhancement; active pharmaceutical ingredients; oral toxicity; confinement; crystallization; pharmaceutical excipients; bioavailability; Inorganic Chemistry; oorganisk kemi;

    Sammanfattning : Poor aqueous solubility is one of the greatest barriers for new drug candidates to enter toxicology studies, let alone clinical trials. This thesis focuses on contributing to solving this problem, evaluating the oral toxicity of mesoporous silica particles, and enhancing the apparent solubility and bioavailability of active pharmaceutical ingredients in vitro and in vivo using mesoporous silica particles. LÄS MER

  4. 4. Membrane Interactions of Arginine-Rich Peptides for the Intracellular Delivery of Gene-Targeted Drugs

    Författare :Per Thoren; Chalmers University of Technology; []
    Nyckelord :cellular uptake; translocation; protein transduction; circular dichroism; drug delivery; liposomes; resonance energy transfer; PNA; antigene; antisense;

    Sammanfattning : A major obstacle for the therapeutic use of e.g. oligonucleotides is their inherently poor cellular uptake. A recently discovered class of peptides, denoted cell-penetrating peptides, has been shown to traverse cell membranes, even when conjugated to oligonucleotides or even full-length proteins. LÄS MER

  5. 5. Toxicological and Immunomodulatory Properties of Mesoporous Silica Particles : Applications in Life Sciences

    Författare :Natalia Kupferschmidt; Alfonso E Garcia-Bennett; Susanne Gabrielsson; Mika Lindén; Uppsala universitet; []
    Nyckelord :ENGINEERING AND TECHNOLOGY; TEKNIK OCH TEKNOLOGIER; mesoporous silica; biocompatibility; adjuvants; drug delivery systems; obesity;

    Sammanfattning : Mesoporous silica particles offer great potential benefits as vehicles for drug delivery and in other biomedical applications. They present a high loading capacity due their ordered and size-tuneable pores that allow molecules to be loaded and released. LÄS MER