Enzyme cleavable nanoparticles from peptide based triblock copolymers

Fuchs, Adrian V., Kotman, Niklas, Andrieu, Julien, Mailänder, Volker, Weiss, Clemens K. and Landfester, Katharina (2013) Enzyme cleavable nanoparticles from peptide based triblock copolymers. Nanoscale, 5 11: 4829-4839. doi:10.1039/c3nr00706e

Author Fuchs, Adrian V.
Kotman, Niklas
Andrieu, Julien
Mailänder, Volker
Weiss, Clemens K.
Landfester, Katharina
Title Enzyme cleavable nanoparticles from peptide based triblock copolymers
Journal name Nanoscale   Check publisher's open access policy
ISSN 2040-3364
Publication date 2013-06-07
Sub-type Article (original research)
DOI 10.1039/c3nr00706e
Open Access Status Not Open Access
Volume 5
Issue 11
Start page 4829
End page 4839
Total pages 11
Place of publication Cambridge, United Kingdom
Publisher Royal Society of Chemistry
Language eng
Formatted abstract
A solid-phase synthesis based approach towards protease cleavable polystyrene–peptide–polystyrene triblock copolymers and their formulation to nanoparticulate systems is presented. These nanoparticles are suitable for the optical detection of an enzyme and have the potential for application as a drug delivery system. Two different peptide sequences, one cleaved by trypsin (GFF), the other by hepsin (RQLRVVGG), a protease overexpressed in early stages of prostate cancer, are used as the central part of the triblock. For optical detection a fluorophore–quencher pair is introduced around the cleavage sequence. The solid phase synthesis is conduced such that two identical sequences are synthesized from one branching point. Eventually, carboxy-terminated polystyrene is introduced into the peptide synthesizer and coupled to the amino-termini of the branched sequence. Upon cleavage, a fragment is released from the triblock copolymer, which has the potential for use in drug delivery applications. Conducting the whole synthesis on a solid phase in the peptide synthesizer avoids solubility issues and post-synthetic purification steps. Due to the hydrophobic PS-chains, the copolymer can easily be formulated to form nanoparticles using a nanoprecipitation process. Incubation of the nanoparticles with the respective enzymes leads to a significant increase of the fluorescence from the incorporated fluorophore, thereby indicating cleavage of the peptide sequence and decomposition of the particles.
Keyword Drug-delivery
Inverse miniemulsion
Q-Index Code C1
Q-Index Status Provisional Code
Institutional Status Non-UQ

Document type: Journal Article
Sub-type: Article (original research)
Collections: Non HERDC
Australian Institute for Bioengineering and Nanotechnology Publications
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Created: Thu, 14 Nov 2013, 07:34:51 EST by Adrian Fuchs on behalf of Aust Institute for Bioengineering & Nanotechnology