Linear and branched polymer prodrugs of the water-soluble nucleoside reverse-transcriptase inhibitor emtricitabine as structural materials for long-acting implants



Shakil, Anika, Hern, Faye Y, Liu, Chung, Temburnikar, Kartik, Chambon, Pierre, Liptrott, Neill ORCID: 0000-0002-5980-8966, McDonald, Tom O ORCID: 0000-0002-9273-9173, Neary, Megan ORCID: 0000-0002-4960-2139, Owen, Andrew ORCID: 0000-0002-9819-7651, Freel Meyers, Caren
et al (show 1 more authors) (2022) Linear and branched polymer prodrugs of the water-soluble nucleoside reverse-transcriptase inhibitor emtricitabine as structural materials for long-acting implants. JOURNAL OF MATERIALS CHEMISTRY B, 10 (23). pp. 4395-4404.

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Linear and branched polymer prodrugs of the water-soluble nucleoside reverse-transcriptase inhibitor emtricitabine as structural materials for long-acting implants, A. Shakil, F. Y. Hern, C. Liu, K. Temburn.pdf - Published version

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Abstract

Long-acting drug delivery is a growing area of interest as it overcomes many challenges related to patient adherence to therapy and the pill burden associated with chronic illness. Injectable formulations are becoming more common and drug-releasing implants also provide several opportunities. Highly water soluble drug compounds are poor candidates for long-acting delivery. Here, the water-soluble nucleoside reverse transcriptase inhibitor emtricitabine (FTC) has been used as a novel A-B monomer in step-growth polymerisation with chloroformate functional C<sub><i>n</i></sub> monomers, to produce new poly(carbamate/carbonate) structures with varying architecture. The polymer prodrugs were all solid at ambient temperature and have been shown to release FTC when subjected to mixed gender human plasma. Vacuum compression moulding has been used to form solid rod implants without polymer degradation; the rods show FTC release over long periods in the presence of microsomes, establishing the basis of a polymer prodrug strategy for FTC delivery.

Item Type: Article
Uncontrolled Keywords: Humans, HIV Infections, Water, Polymers, DNA-Directed RNA Polymerases, Nucleosides, Prodrugs, Reverse Transcriptase Inhibitors, Anti-HIV Agents, Emtricitabine
Divisions: Faculty of Health and Life Sciences
Faculty of Health and Life Sciences > Institute of Systems, Molecular and Integrative Biology
Faculty of Science and Engineering > School of Physical Sciences
Depositing User: Symplectic Admin
Date Deposited: 11 Jul 2022 14:10
Last Modified: 18 Jan 2023 20:56
DOI: 10.1039/d2tb00825d
Related URLs:
URI: https://livrepository.liverpool.ac.uk/id/eprint/3158056