Issue 12, 2020
From the journal:

Organic & Biomolecular Chemistry

Functionalised thermally induced phase separation (TIPS) microparticles enabled for “click” chemistry†

João C. F. Nogueira,a   Ketevan Paliashvili,b   Alexandra Bradford,b   Francesco Di Maggio,b   Daniel A. Richards,a   Richard M. Day*bc  and  Vijay Chudasama ORCID logo *a  

* Corresponding authors

a UCL Chemistry Department, University College London, Gower Street, London, UK
E-mail: v.chudasama@ucl.ac.uk

b Centre for Precision Healthcare, UCL Division of Medicine, University College London, Gower Street, London, UK
E-mail: r.m.day@ucl.ac.uk

c The Discoveries Centre for Regenerative and Precision Medicine, University College London, Gower Street, London, UK

Abstract

Due to their homogeneity, tuneable properties, low cost and ease of manufacture, thermally induced phase separation (TIPS) polymeric microparticles are emerging as an exciting class of injectable device for the treatment of damaged tissue or complex diseases, such as cancer. However, relatively little work has explored enhancing surface functionalisation of this system. Herein, we present the functionalisation of TIPS microparticles with both small molecules and an antibody fragment of Herceptin™, via a heterobifunctional pyridazinedione linker capable of participating in SPAAC “click” chemistry, and compare it to the traditional method of preparing active-targeted microparticle systems, that is, physisorption of antibodies to the microparticle surface. Antigen-binding assays demonstrated that functionalisation of microparticles with Herceptin Fab, via a pyridazinedione linker, provided an enhanced avidity to HER2+ when compared to traditional physisorption methods.

Graphical abstract: Functionalised thermally induced phase separation (TIPS) microparticles enabled for “click” chemistry

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Article information

DOI
https://doi.org/10.1039/D0OB00106F
Article type
Communication
Submitted
17 Jan 2020
Accepted
02 Mar 2020
First published
02 Mar 2020
This article is Open Access
Creative Commons BY license

Org. Biomol. Chem., 2020,18, 2215-2218

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Functionalised thermally induced phase separation (TIPS) microparticles enabled for “click” chemistry

J. C. F. Nogueira, K. Paliashvili, A. Bradford, F. Di Maggio, D. A. Richards, R. M. Day and V. Chudasama, Org. Biomol. Chem., 2020, 18, 2215 DOI: 10.1039/D0OB00106F

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