Towards Targeted Drug Delivery by Covalent Ligand-Modified Polymeric Nanocontainers |
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Authors: | Stefan Egli Barbara Fischer Sonja Hartmann Patrick Hunziker Wolfgang Meier Per Rigler |
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Institution: | 1. Physikalische Chemie, Universität Basel, Klingelbergstrasse 80, 4056 Basel, Switzerland;2. Medical Intensive Care Unit, University Hospital Basel, Petersgraben 4, 4031 Basel, Switzerland |
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Abstract: | Here we present a novel strategy for specific cellular targeting of polymeric nanocontainers by using self-assembly of block copolymers consisting of either Polydimethoxysiloxane-b-Polymethyloxazoline-b-Polydimethoxysiloxane (PDMS-b-PMOXA-b-PDMS) or functionalized PDMS-b-PMOXA-b-PDMS. Covalent functionalization of the above copolymer was accomplished using either the fluorescent dye sulforhodamine B or a poly-guanosin ligand, the latter by using the Huisgen 1,3-dipolar cycloaddition. The success of the covalent modification of the block copolymer has been determined by studying functionalized sulforhodamine B by NMR and fluorescence correlation spectroscopy. The covalent click chemistry approach leads to efficiently functionalized polymeric nanocontainers which enables specific uptake by activated macrophages overexpressing the scavenger receptor A1. |
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Keywords: | block copolymers drug delivery systems fluorescence functionalization of polymers nanoparticles |
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