Institute of Pharmacy and Pharmacology, Hunan Province Cooperative Innovation Center for Molecular Target New Drug Study, University of South China, Hengyang, China.
Xiangya School of Pharmaceutical Sciences, Central South University, Changsha, China.
Int J Pharm. 2018 Jan 15;535(1-2):253-260. doi: 10.1016/j.ijpharm.2017.11.003. Epub 2017 Nov 4.
During the past decades, chemotherapy has been regarded as the most effective method for tumor therapy, but still faces significant challenges, such as poor tumor selectivity and multidrug resistance. The development of targeted drug delivery systems brings certain dramatic advantages for reducing the side effects and improving the therapeutic efficacy. Coupling a specific stimuli-triggered drug release mechanism with these delivery systems is one of the most prevalent approaches for targeted therapy. Among these approaches, pH-sensitive micelles are regarded as the most general strategy with advantages of increasing solubility of water-insoluble drugs, pH-sensitive release, high drug loading, etc. This review will focus on the potential of pH-sensitive micelles in tumor therapy, analyze four types of drug-loaded micelles and mechanisms of drug release and give an exhaustive collection of recent investigations. Sufficient understanding of these mechanisms will help us to design more efficient pH-sensitive drug delivery system to address the challenges encountered in targeted drug delivery systems for tumor therapy.
在过去几十年中，化疗被认为是肿瘤治疗最有效的方法，但仍面临着许多挑战，如肿瘤选择性差和多药耐药性。靶向药物传递系统的发展为降低副作用和提高治疗效果带来了一定的显著优势。将特定的刺激触发药物释放机制与这些传递系统相结合是靶向治疗的最常见方法之一。在这些方法中，pH 敏感胶束被认为是最通用的策略，具有增加水不溶性药物的溶解度、pH 敏感释放、高载药量等优点。本文综述了 pH 敏感胶束在肿瘤治疗中的应用潜力，分析了四种载药胶束的类型和药物释放机制，并对最近的研究进行了全面的收集。充分了解这些机制将有助于我们设计更有效的 pH 敏感药物传递系统，以解决肿瘤治疗中靶向药物传递系统所遇到的挑战。
