Pharmacokinetics of polymersomes composed of poly(Butadiene-Ethylene Oxide); Healthy versus tumor-bearing mice

Journal article (2016)

Authors

G Wang RST/Radiation, Science and Technology , Old organisation ChemE/Phys.Chem. & Mol.Thermod.
R.M. de Kruijff RST/Applied Radiation & Isotopes - AS , RST/Radiation, Science and Technology
DS Abou Division of Nuclear Medicine, Johns Hopkins Hospital, RST/Applied Radiation & Isotopes - AS
NN Ramos Memorial Sloan-Kettering Cancer Center
E. Mendes ChemE/Advanced Soft Matter - AS
L. E. Franken University Medical Center Groningen
H.T. Wolterbeek RST/Radiation, Science and Technology
A.G. Denkova RST/Radiation, Science and Technology , RST/Applied Radiation & Isotopes - AS
Research Group
ChemE/Advanced Soft Matter (AS) (TU Delft)
In Healthy and Tumour Bearing Mice MicroSPECT Pharmacokinetics and Biodistribution Radiolabeled Polymersomes
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Published Date

01-02-2016

Language

English

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Faculty

Applied Sciences

Department

ChemE/Chemical Engineering

Research Group

ChemE/Advanced Soft Matter

Abstract

Vesicles composed of block copolymers (i.e., polymersomes) are one of the most versatile nano-carriers for medical purposes due to their tuneable physicochemical properties and the possibility to encapsulate simultaneously hydrophobic and hydrophilic substances, allowing, for instance, the combination of therapy and imaging. In cancer treatment, these vesicles need to remain long enough in the blood stream to be sufficiently taken up by tumors. Here, we have investigated the biodistribution and the pharmacokinetics of polymersomes, composed of poly(butadiene-b-ethylene oxide) having dimensions around 80 nm. The polymersomes have been radiolabeled with 111In via the so-called active loading method achieving a loading efficiency of 92.9±0.9% with radionuclide retention in mouse serum of more than 95% at 24 h. The optimized 111In containing polymersomes have been intravenously administered in healthy and tumor bearing mice for pharmacokinetic determination using microSPECT (Single Photon Emission Computed Tomography). In healthy mice these polymersomes have been found to exhibit relatively long blood circulation (>6 h), low liver uptake (6±1.5%ID/g, 48 h p.i.) and elevated spleen uptake (188±30%ID/g). The blood circulation in tumor bearing mice is dramatically reduced (