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The Synthesis of Peptide-Conjugated Poly(2-Ethyl-2-Oxazoline)-bpoly(L-Lactide) (PEtOx-B-PLA) Polymeric Systems Through the Combination of Controlled Polymerization Techniques and Click Reactions

preprint
submitted on 23.06.2020 and posted on 25.06.2020 by Umut Ugur Ozkose, Sevgi Gulyuz, Melek Parlak Khalily, Salih Ozcubukcu, Asuman Bozkır, Mehmet Atilla Taşdelen, onur alpturk, Özgür Yılmaz
To optimize the therapeutic effect of pharmaceutical agents, drug delivery systems tailored from FDA-approved polymers like poly(L-lactide) (PLA) is an effective strategy. Because of their hydrophobic character, these systems greatly suffer from reduced circulation time thus, amphiphilic block copolymers became favourable to overcome this limitation. Of them, poly(oxazoline)-b-poly(L-lactide) are of choice as poly(oxazoline) (PEtOx) is compatibile, biodegradable, while exhibiting minimum cytotoxicity. To tailor selective drug targeting drug delivery systems, whereby their selectivity for tumour tissues is maximised, these polymers should be decorated with so-called tumour-homing agents, such as antibodies, peptides and so forth. To this respect, we designed a new block copolymer, allyl-poly(2-ethyl-2-oxazoline)-b-poly(L-lactide) allyl-(PEtOx-b-PLA) and its subsequent conjugation to tumour-homing peptides, peptide-18 and peptide-563 at the terminal position. In this manuscript, we report our synthetic route to obtain this building block and its conjugation to tumour-homing agents.

Funding

This research is supported by the Scientific and Technological Research Council of Turkey (TUBITAK) (grant number: 213M725).

History

Email Address of Submitting Author

yilmaz.ozgur@tubitak.gov.tr

Institution

Materials Institute, Marmara Research Center, TUBITAK, Kocaeli

Country

Turkey

ORCID For Submitting Author

https://orcid.org/0000-0003-3892-2775

Declaration of Conflict of Interest

No conflict of interest

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