Abstract
To determine the fate of polymeric micelles after oral administration, we investigated the possible transport of polymeric micelles across Caco-2 monolayers and their biodistribution in rats after per os administration of [14C]-labelled mmePEG750P(CL-co-TMC) micelles containing risperidone (BCS Class II drug). mmePEG750P(CL-co-TMC) was able to cross Caco-2 monolayer via a saturable transport mechanism. The oral bioavailability of the polymer was 40%. Polymeric micelles based on mmePEG750P(CL-co-TMC) showed very low clearance by the reticuloendothelial system (RES) and a renal excretion. A sustained release of risperidone was observed.
Publication types
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Comparative Study
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Research Support, Non-U.S. Gov't
MeSH terms
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Administration, Oral
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Animals
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Antipsychotic Agents / administration & dosage
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Antipsychotic Agents / blood
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Antipsychotic Agents / pharmacokinetics
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Area Under Curve
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Biological Availability
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Biological Transport
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Caco-2 Cells
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Carbon Radioisotopes
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Enterocytes / metabolism
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Humans
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Injections, Intravenous
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Intestinal Absorption*
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Isoxazoles / blood
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Kidney / metabolism
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Male
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Metabolic Clearance Rate
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Micelles*
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Mononuclear Phagocyte System / metabolism
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Paliperidone Palmitate
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Polyesters / administration & dosage
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Polyesters / chemical synthesis
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Polyesters / pharmacokinetics*
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Polyethylene Glycols / administration & dosage
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Polyethylene Glycols / chemical synthesis
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Polyethylene Glycols / pharmacokinetics*
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Polymers / administration & dosage
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Polymers / chemical synthesis
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Polymers / pharmacokinetics*
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Pyrimidines / blood
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Rats
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Rats, Sprague-Dawley
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Risperidone / administration & dosage
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Risperidone / blood
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Risperidone / pharmacokinetics
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Tissue Distribution
Substances
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Antipsychotic Agents
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Carbon Radioisotopes
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Isoxazoles
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Micelles
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Polyesters
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Polymers
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Pyrimidines
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monomethyletherpoly(oxyethylene glycol(750))-poly(caprolactone-co-trimethylene carbonate)
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Polyethylene Glycols
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Risperidone
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Paliperidone Palmitate