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Mol Pharm. 2016 Mar 7;13(3):1158-65. doi: 10.1021/acs.molpharmaceut.5b00958. Epub 2016 Feb 25.

SPECT/CT Imaging of Pluronic Nanocarriers with Varying Poly(ethylene oxide) Block Length and Aggregation State.

Author information

1
Institut Charles Sadron (CNRS), Strasbourg, France.
2
Department of Radiation Science and Technology, Delft University of Technology , 2629 JB Delft, The Netherlands.
3
MILabs B.V., 3584 CX Utrecht, The Netherlands.
4
Department of Translational Neuroscience, Brain Center Rudolf Magnus, University Medical Center , 3584 CG Utrecht, The Netherlands.
5
Department of Organic and Macromolecular Chemistry, Ghent University , B-9000 Ghent, Belgium.
6
Department of Chemical Engineering, Delft University of Technology , 2628 BL Delft, The Netherlands.

Abstract

Optimal biodistribution and prolonged circulation of nanocarriers improve diagnostic and therapeutic effects of enhanced permeability and retention-based nanomedicines. Despite extensive use of Pluronics in polymer-based pharmaceuticals, the influence of different poly(ethylene oxide) (PEO) block length and aggregation state on the biodistribution of the carriers is rather unexplored. In this work, we studied these effects by evaluating the biodistribution of Pluronic unimers and cross-linked micelles with different PEO block size. In vivo biodistribution of (111)In-radiolabeled Pluronic nanocarriers was investigated in healthy mice using single photon emission computed tomography. All carriers show fast uptake in the organs from the reticuloendothelial system followed by a steady elimination through the hepatobiliary tract and renal filtration. The PEO block length affects the initial renal clearance of the compounds and the overall liver uptake. The aggregation state influences the long-term accumulation of the nanocarriers in the liver. We showed that the circulation time and elimination pathways can be tuned by varying the physicochemical properties of Pluronic copolymers. Our results can be beneficial for the design of future Pluronic-based nanomedicines.

KEYWORDS:

Pluronic; SPECT; micelles; unimers

[Indexed for MEDLINE]

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