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

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...

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

“…There is also considerable potential for the synthesis of backbone copolymers, to blend carbonate and ester links, and copolymers derived from mixed monomers containing variation in carbamate chemistry. When compared to our previous reports of polymers containing FTC within the backbone, 26 we have a considerably slower release of parent drug during activation which may be highly important when evaluating these approaches in vivo .…”

“…1(B) and (C), were readily previously synthesised using mono-or bis-chloroformates with varying structures. 20,26 The resulting carbonate and carbamate links were known enzymatic substrates and activation to parent FTC was expected to occur under appropriate conditions. The carbamate linking group has previously been utilised in the chemistry of capecitabine, a prodrug of 5-fluorouracil, 27 and the 5-flucytosine ring is common to FTC.…”

“…The four polymers 8a polycarb(Et- n Bu), 8b polycarb(Et-iBu), 10a polyester(Glu- n Bu), and 10b polyester(Glu-iBu) were, therefore, subjected to vacuum compression moulding (VCM) as previously described. 26 In summary, the powdered polymers were loaded into a silicone tube that was mounted within a VCM mould, and sandwiched between PTFE release foils, Fig. 10(A) .…”

Synthesis, Characterization, and Evaluation of Antioxidant and Physical Properties of New Bifunctional Aromatic Monomers Containing Imine and Heterocyclic Rings in The Main Chain.

“…Monomers are distinguished from other organic compounds in their containing bi-functional groups instead of one. This leads to the formation of linear polymers 13,14 , while if they include more than two functional groups, it will lead to the formation of a branched polymer, and each of the polymers has its applications and uses 15,16 . Oxazepanes are Heterocyclic compounds with a seven-ring ring 17 that contain lactone(O-C=O) and lactam (HN-C=O) 18 .…”