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Issue 8, 2009
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Polymeric nanocontainers with high loading capacity of hydrophobic drugs

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Abstract

Water soluble 4- and 6-arm star-shaped polymers with (bio)degradable hydrophobic cores and dense hydrophilic coronas were synthesized by a combination of ring opening polymerization (ROP) and atom transfer radical polymerization (ATRP). Their carrier abilities of different model compounds as well as active pharmaceutically ingredients in aqueous solutions were evaluated by UV/Vis and 1H NMR spectroscopy studies. The highest loading capacities (up to 36 guest molecules per molecule of polymer) were, as expected, found for the 6-arm star-shaped polymers. The densely grafted poly[poly(ethylene glycol)methyl ether methacrylate] [p(mPEGMA)] shell stabilizes the host–guest complexes preventing undesired multimolecular aggregation. Dynamic light scattering (DLS) measurements evidenced the unimolecular character of all 4- and 6-arm polymers before and after loading with guest molecules. The (bio)degradability of the core was demonstrated under acidic conditions and in vitro using a lipase from Rhizopus Arrhizus. The dual-stimuli responsiveness of the hydrophobic core to enzymes and pH may facilitate increased control over in vivo drug release.

Graphical abstract: Polymeric nanocontainers with high loading capacity of hydrophobic drugs

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Supplementary files

Article information


Submitted
15 Sep 2008
Accepted
16 Jan 2009
First published
02 Mar 2009

Soft Matter, 2009,5, 1662-1667
Article type
Paper

Polymeric nanocontainers with high loading capacity of hydrophobic drugs

O. G. Schramm, M. A. R. Meier, R. Hoogenboom, H. P. van Erp, J. Gohy and U. S. Schubert, Soft Matter, 2009, 5, 1662
DOI: 10.1039/B816087B

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