School of Biological Science and Technology, University of Jinan, No. 336 West Road of Nanxinzhuang, Jinan 250022, Shandong Province, China.
Anticancer Agents Med Chem. 2020;20(18):2169-2189. doi: 10.2174/1871520620666200719001038.
Paclitaxel (PTX) has been clinically used for several years due to its good therapeutic effect against cancers. Its poor water-solubility, non-selectivity, high cytotoxicity to normal tissue and worse pharmacokinetic property limit its clinical application.
To review the recent progress on the PTX delivery systems.
In recent years, the copolymeric nano-drug delivery systems for PTX are broadly studied. It mainly includes micelles, nanoparticles, liposomes, complexes, prodrugs and hydrogels, etc. They were developed or further modified with target molecules to investigate the release behavior, targeting to tissues, pharmacokinetic property, anticancer activities and bio-safety of PTX. In the review, we will describe and discuss the recent progress on the nano-drug delivery system for PTX since 2011.
The water-solubility, selective delivery to cancers, tissue toxicity, controlled release and pharmacokinetic property of PTX are improved by its encapsulation into the nano-drug delivery systems. In addition, its activities against cancer are also comparable or high when compared with the commercial formulation.
Encapsulating PTX into nano-drug carriers should be helpful to reduce its toxicity to human, keeping or enhancing its activity and improving its pharmacokinetic property.
紫杉醇(PTX)由于对癌症具有良好的治疗效果,已在临床上应用多年。但其水溶性差、非选择性、对正常组织的细胞毒性高和药代动力学性质差限制了其临床应用。
综述 PTX 给药系统的最新研究进展。
近年来,用于 PTX 的共聚纳米药物传递系统得到了广泛的研究。它主要包括胶束、纳米粒、脂质体、复合物、前药和水凝胶等,通过与靶向分子的开发或进一步修饰,研究 PTX 的释放行为、组织靶向性、药代动力学特性、抗癌活性和生物安全性。在本综述中,我们将描述和讨论自 2011 年以来 PTX 纳米药物传递系统的最新研究进展。
将 PTX 包封到纳米药物传递系统中可以提高其水溶性、对癌症的选择性传递、组织毒性、控制释放和药代动力学特性。此外,其抗癌活性与商业制剂相当或更高。
将 PTX 包封到纳米药物载体中有助于降低其对人体的毒性,保持或增强其活性,改善其药代动力学特性。