Issue 31, 2017

Precise control of drug loading and release of an NSAID–polymer conjugate for long term osteoarthritis intra-articular drug delivery

Abstract

A facile synthesis method of polymer diclofenac conjugates (PDCs) based on biocompatible polyurethane chemistry that provides a high drug loading and offers a high degree of control over diclofenac (DCF) release kinetics is described. DCF incorporating monomer was reacted with ethyl-L-lysine diisocyanate (ELDI) and different amounts of polyethylene glycol (PEG) in a one-step synthesis to yield polymers with pendent diclofenac distributed along the backbone. By adjusting the co-monomers feed ratio, the drug loading could be tailored accordingly to give DCF loading of up to 38 w/w%. The release rate could also be controlled easily by changing the amount of PEG in the backbone. Above 10 w/w% of PEG, the in vitro DCF release studies in physiological conditions showed an apparent zero-order profile without an initial burst effect for up to 120 days. The PDCs described may be suitable for long-term intra-articular (IA) delivery for the treatment of osteoarthritis (OA).

Graphical abstract: Precise control of drug loading and release of an NSAID–polymer conjugate for long term osteoarthritis intra-articular drug delivery

Supplementary files

Article information

Article type
Communication
Submitted
06 Jun 2017
Accepted
24 Jul 2017
First published
24 Jul 2017

J. Mater. Chem. B, 2017,5, 6221-6226

Precise control of drug loading and release of an NSAID–polymer conjugate for long term osteoarthritis intra-articular drug delivery

A. Sulistio, F. Reyes-Ortega, A. M. D’Souza, S. M. Y. Ng, D. Valade, J. F. Quinn, A. C. Donohue, F. Mansfeld, A. Blencowe, G. Qiao, R. Prankerd, S. Quirk, M. R. Whittaker, T. P. Davis and R. J. Tait, J. Mater. Chem. B, 2017, 5, 6221 DOI: 10.1039/C7TB01518F

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