Serras Ana, Faustino Célia, Pinheiro Lídia
Research Institute for Medicines (iMed.ULisboa), Faculdade de Farmácia, Universidade de Lisboa (ULisboa), Avenida Professor Gama PintoGama Pinto, 1649-003 Lisboa, Portugal.
Pharmaceutics. 2024 Aug 6;16(8):1047. doi: 10.3390/pharmaceutics16081047.
Cancer is still ranked among the top three causes of death in the 30- to 69-year-old age group in most countries and carries considerable societal and macroeconomic costs that differ depending on the cancer type, geography, and patient gender. Despite advances in several pharmacological approaches, the lack of stability and specificity, dose-related toxicity, and limited bioavailability of chemotherapy (standard therapy) pose major obstacles in cancer treatment, with multidrug resistance being a driving factor in chemotherapy failure. The past three decades have been the stage for intense research activity on the topic of nanomedicine, which has resulted in many nanotherapeutics with reduced toxicity, increased bioavailability, and improved pharmacokinetics and therapeutic efficacy employing smart drug delivery systems (SDDSs). Polymeric micelles (PMs) have become an auspicious DDS for medicinal compounds, being used to encapsulate hydrophobic drugs that also exhibit substantial toxicity. Through preclinical animal testing, PMs improved pharmacokinetic profiles and increased efficacy, resulting in a higher safety profile for therapeutic drugs. This review focuses on PMs that are already in clinical trials, traveling the pathways from preclinical to clinical studies until introduction to the market.
在大多数国家，癌症仍是30至69岁年龄组中排名前三的死因之一，且会带来相当大的社会和宏观经济成本，这些成本因癌症类型、地理位置和患者性别而异。尽管在几种药理学方法上取得了进展，但化疗（标准疗法）缺乏稳定性和特异性、与剂量相关的毒性以及有限的生物利用度，在癌症治疗中构成了重大障碍，其中多药耐药性是化疗失败的一个驱动因素。过去三十年一直是纳米医学领域密集研究活动的阶段，这导致了许多纳米疗法的出现，这些纳米疗法利用智能药物递送系统（SDDSs）降低了毒性、提高了生物利用度，并改善了药代动力学和治疗效果。聚合物胶束（PMs）已成为一种用于药用化合物的理想药物递送系统，用于封装也具有相当大毒性的疏水性药物。通过临床前动物试验，PMs改善了药代动力学特征并提高了疗效，从而提高了治疗药物的安全性。本综述重点关注已进入临床试验的PMs，它们正沿着从临床前研究到临床研究直至推向市场的路径发展。
