Bernabeu Ezequiel, Cagel Maximiliano, Lagomarsino Eduardo, Moretton Marcela, Chiappetta Diego A
Universidad de Buenos Aires, Facultad de Farmacia y Bioquímica, Cátedra de Tecnología Farmacéutica I, Buenos Aires, Argentina; Consejo Nacional de Investigaciones Científicas y Técnicas (CONICET), Argentina.
Universidad de Buenos Aires, Facultad de Farmacia y Bioquímica, Cátedra de Tecnología Farmacéutica I, Buenos Aires, Argentina; Consejo Nacional de Investigaciones Científicas y Técnicas (CONICET), Argentina.
Int J Pharm. 2017 Jun 30;526(1-2):474-495. doi: 10.1016/j.ijpharm.2017.05.016. Epub 2017 May 10.
In recent years, the nanotechnology has offered researchers the opportunity to solve the problems caused by the vehicle of the standard and first formulation of paclitaxel (Taxol), while maximizing the proven antineoplastic activity of the drug against many solid tumors. Hence, different types of nanocarriers have been employed to improve the efficacy, safety, physicochemical properties and pharmacokinetic/pharmacodynamic profile of this drug. To date, paclitaxel is the unique drug that is marketed in three different nanoplatforms for its parenteral delivery: polymeric nanoparticles (Abraxane), liposomes (Lipusu), and polymeric micelles (Genexol, Nanoxel and Paclical). Indeed, a fourth nanocarrier might be available soon, because phase III studies of Opaxio™, a polymeric-conjugated, are near completion. Furthermore, other several nanoformulations are currently in various stages of clinical trials. Therefore, it is only through the critical analysis of clinical evidence from these studies that we can get a more concrete idea of what has been achieved with pharmaceutical nanotechnology so far. This review attempts to summarize current information available regarding the clinical status and the physicochemical characteristic of different nanocarriers for paclitaxel delivery in cancer therapy. We present an overview of the preclinical and clinical data of these systems including their pharmacokinetics, dose and administration, adverse events and clinical efficacy.
近年来，纳米技术为研究人员提供了机会，以解决由紫杉醇（泰素）标准及最初剂型的载体所引发的问题，同时使该药物对多种实体瘤已被证实的抗肿瘤活性最大化。因此，已采用不同类型的纳米载体来提高这种药物的疗效、安全性、理化性质以及药代动力学/药效学特征。迄今为止，紫杉醇是唯一一种以三种不同纳米平台进行肠胃外给药销售的药物：聚合物纳米粒（Abraxane）、脂质体（力朴素）和聚合物胶束（Genexol、Nanoxel和Paclical）。事实上，可能很快会有一种新的纳米载体出现，因为聚合物缀合物Opaxio™的III期研究已接近完成。此外，其他几种纳米制剂目前正处于临床试验的不同阶段。因此，只有通过对这些研究的临床证据进行批判性分析，我们才能更具体地了解到目前药物纳米技术已取得的成果。本综述试图总结目前关于癌症治疗中用于递送紫杉醇的不同纳米载体的临床状况和理化特性的可用信息。我们概述了这些系统的临床前和临床数据，包括它们的药代动力学、剂量与给药、不良事件和临床疗效。
