Grosso Roberto, de-Paz M-Violante
Departamento Química Orgánica y Farmacéutica, Facultad de Farmacia, Universidad de Sevilla, 41012 Sevilla, Spain.
Pharmaceutics. 2021 Jun 8;13(6):854. doi: 10.3390/pharmaceutics13060854.
Thiomers (or thiolated polymers) have broken through as avant-garde approaches in anticancer therapy. Their distinguished reactivity and properties, closely linked to their final applications, justify the extensive research conducted on their preparation and use as smart drug-delivery systems (DDSs). Multiple studies have demonstrated that thiomer-rich nanoformulations can overcome major drawbacks found when administering diverse active pharmaceutical ingredients (APIs), especially in cancer therapy. This work focuses on providing a complete and concise review of the synthetic tools available to thiolate cationic and anionic polymers, in particular chitosan (CTS) and hyaluronic acid (HA), respectively, drawing attention to the most successful procedures. Their chemical reactivity and most relevant properties regarding their use in anticancer formulations are also discussed. In addition, a variety of NP formation procedures are outlined, as well as their use in cancer therapy, particularly for taxanes and siRNA. It is expected that the current work could clarify the main synthetic strategies available, with their scope and drawbacks, as well as provide some insight into thiomer chemistry. Therefore, this review can inspire new research strategies in the development of efficient formulations for the treatment of cancer.
硫醇聚合物(或硫醇化聚合物)已成为抗癌治疗中的前沿方法。它们独特的反应活性和性质与其最终应用密切相关,这使得人们对其作为智能药物递送系统(DDS)的制备和应用进行了广泛研究。多项研究表明,富含硫醇聚合物的纳米制剂能够克服在施用多种活性药物成分(API)时发现的主要缺点,尤其是在癌症治疗中。本文着重对可用于硫醇化阳离子和阴离子聚合物(特别是壳聚糖(CTS)和透明质酸(HA))的合成工具进行全面而简洁的综述,重点关注最成功的方法。还讨论了它们的化学反应活性以及在抗癌制剂中的最相关性质。此外,概述了多种纳米颗粒形成方法及其在癌症治疗中的应用,特别是用于紫杉烷类和小干扰RNA(siRNA)。期望当前的工作能够阐明可用的主要合成策略及其范围和缺点,并为硫醇聚合物化学提供一些见解。因此,本综述能够激发在开发高效癌症治疗制剂方面的新研究策略。