Issue 7, 2015

Well-defined diblock brush polymer–drug conjugates for sustained delivery of paclitaxel

Abstract

Using the 3rd generation Grubbs’ catalyst as the initiator, diblock brush polymer drug conjugates (BPDCs) were synthesized by sequential ring-opening metathesis polymerization (ROMP) of a hydrophilic poly(ethylene glycol) (PEG)-based norbornene (NB)-functionalized macromonomer and a hydrophobic paclitaxel (PTXL)-based NB-functionalized monomer. These amphiphilic diblock BPDCs had well-defined structures, with narrow molecular weight distributions (Mw/Mn = 1.10–1.16). They self-assembled into multi-molecular nanostructures in aqueous solutions. Although the PTXL moieties were connected to the backbone with cycloacetal-based conjugation linkages, the cleavage of these linkages from the assemblies of diblock BPDCs was relatively slow and exhibited limited acid-sensitivity, indicating a significant influence of the macromolecular structure and assembly of BPDCs on their drug release behaviour. The cytotoxicity study not only showed that the diblock BPDCs are therapeutically effective against cancer cells, but also revealed a correlation between cytotoxicity and grafting structures of BPDCs. In summary, the results obtained in this work provide new insight into the structure-dependent properties of brush polymer-based drug delivery systems.

Graphical abstract: Well-defined diblock brush polymer–drug conjugates for sustained delivery of paclitaxel

Supplementary files

Article information

Article type
Paper
Submitted
29 dec 2014
Accepted
29 jan 2015
First published
11 feb 2015

Biomater. Sci., 2015,3, 1078-1084

Author version available

Well-defined diblock brush polymer–drug conjugates for sustained delivery of paclitaxel

J. Zou, Y. Yu, Y. Li, W. Ji, C. Chen, W. Law, P. N. Prasad and C. Cheng, Biomater. Sci., 2015, 3, 1078 DOI: 10.1039/C4BM00458B

To request permission to reproduce material from this article, please go to the Copyright Clearance Center request page.

If you are an author contributing to an RSC publication, you do not need to request permission provided correct acknowledgement is given.

If you are the author of this article, you do not need to request permission to reproduce figures and diagrams provided correct acknowledgement is given. If you want to reproduce the whole article in a third-party publication (excluding your thesis/dissertation for which permission is not required) please go to the Copyright Clearance Center request page.

Read more about how to correctly acknowledge RSC content.

Social activity

Spotlight

Advertisements