Department of Drug Science and Technology, University of Turin, Via P. Giuria 9, 10125, Turin, Italy.
Drug Deliv Transl Res. 2022 Aug;12(8):1911-1927. doi: 10.1007/s13346-022-01127-4. Epub 2022 Feb 25.
Pentamidine (PTM), which is a diamine that is widely known for its antimicrobial activity, is a very interesting drug whose mechanism of action is not fully understood. In recent years, PTM has been proposed as a novel potential drug candidate for the treatment of mental illnesses, myotonic dystrophy, diabetes, and tumors. Nevertheless, the systemic administration of PTM causes severe side effects, especially nephrotoxicity. In order to efficiently deliver PTM and reduce its side effects, several nanosystems that take advantage of the chemical characteristics of PTM, such as the presence of two positively charged amidine groups at physiological pH, have been proposed as useful delivery tools. Polymeric, lipidic, inorganic, and other types of nanocarriers have been reported in the literature for PTM delivery, and they are all in different development phases. The available approaches for the design of PTM nanoparticulate delivery systems are reported in this review, with a particular emphasis on formulation strategies and in vitro/in vivo applications. Furthermore, a critical view of the future developments of nanomedicine for PTM applications, based on recent repurposing studies, is provided. Created with BioRender.com.
戊二脒(PTM)是一种广泛应用于抗菌的二脒类化合物,它是一种非常有趣的药物,其作用机制尚未完全阐明。近年来,PTM 被提议作为一种新型的潜在药物候选物,用于治疗精神疾病、肌强直性营养不良、糖尿病和肿瘤。然而,PTM 的全身给药会引起严重的副作用,尤其是肾毒性。为了高效地输送 PTM 并降低其副作用,已经提出了几种利用 PTM 的化学特性的纳米系统,例如在生理 pH 下存在两个带正电荷的脒基。在文献中已经报道了用于 PTM 递送的聚合物、脂质体、无机和其他类型的纳米载体,它们都处于不同的开发阶段。本文综述了 PTM 纳米颗粒递药系统的设计方法,重点介绍了制剂策略和体外/体内应用。此外,根据最近的再利用研究,对基于纳米医学的 PTM 应用的未来发展进行了批判性的讨论。由 BioRender.com 创建。