Issue 48, 2023

Polymer–prodrug conjugates as candidates for degradable, long-acting implants, releasing the water-soluble nucleoside reverse-transcriptase inhibitor emtricitabine

Abstract

Circulating, soluble polymer–drug conjugates have been utilised for many years to aid the delivery of sensitive, poorly-soluble or cytotoxic drugs, prolong circulation times or minimise side effects. Long-acting therapeutics are increasing in their healthcare importance, with intramuscular and subcutaneous administration of liquid formulations being most common. Degradable implants also offer opportunities and the use of polymer–prodrug conjugates as implant materials has not been widely reported in this context. Here, the potential for polymer–prodrug conjugates of the water soluble nucleoside reverse transciption inhibitor emtricitabine (FTC) is studied. A novel diol monomer scaffold, allowing variation of prodrug substitution, has been used to form polyesters and polycarbonates by step-growth polymerisation. Materials have been screened for physical properties that enable implant formation, studied for drug release to provide mechanistic insights, and tunable prolonged release of FTC has been demonstrated over a period of at least two weeks under relevant physiological conditions.

Graphical abstract: Polymer–prodrug conjugates as candidates for degradable, long-acting implants, releasing the water-soluble nucleoside reverse-transcriptase inhibitor emtricitabine

Supplementary files

Article information

Article type
Paper
Submitted
28 Sep 2023
Accepted
06 Nov 2023
First published
07 Nov 2023
This article is Open Access
Creative Commons BY license

J. Mater. Chem. B, 2023,11, 11532-11543

Polymer–prodrug conjugates as candidates for degradable, long-acting implants, releasing the water-soluble nucleoside reverse-transcriptase inhibitor emtricitabine

C. Liu, F. Y. Hern, A. Shakil, K. Temburnikar, P. Chambon, N. Liptrott, T. O. McDonald, M. Neary, C. Flexner, A. Owen, C. F. Meyers and S. P. Rannard, J. Mater. Chem. B, 2023, 11, 11532 DOI: 10.1039/D3TB02268D

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