Linear and branched polymer prodrugs of the water-soluble nucleoside reverse-transcriptase inhibitor emtricitabine as structural materials for long-acting implants.
Linear and branched polymer prodrugs of the water-soluble nucleoside reverse-transcriptase inhibitor emtricitabine as structural materials for long-acting implants.
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DOI：
10.1039/d2tb00825d
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发表时间：
2022-06-15
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长效给药是一个越来越受关注的领域，因为它克服了与患者坚持治疗和慢性病相关的药片负担有关的许多挑战。注射制剂正变得越来越普遍，药物释放植入物也提供了几个机会。高度水溶性的药物化合物不太适合长效给药。在这里，水溶性核苷逆转录酶抑制剂恩曲他滨(FTC)被用作一种新型的A-B单体，与氯甲酸酯功能CN单体进行逐步聚合，以合成不同结构的新型聚氨基甲酸酯/碳酸酯结构。这些聚合物前药在常温下都是固体，并已被证明在混合性别的人血浆中释放FTC。真空压缩模塑已被用于形成固体棒植入物而不会降解聚合物；棒在微生物体存在的情况下表现出长时间的FTC释放，为FTC释放的聚合物前药战略奠定了基础。以水溶性核苷逆转录酶抑制剂恩曲他滨(FTC)为单体，通过形成聚合物和用含药聚合物制成植入物，在体外证明了FTC的长效释放。
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 Cn 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. Long acting release of the water soluble nucleoside reverse transcriptase inhibitor emtricitabine (FTC) has been demonstrated in vitro through polymer formation using FTC as a monomer, and forming implants made of the drug containing polymer.
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