Key Laboratory for Biorheological Science and Technology of Ministry of Education, State and Local Joint Engineering Laboratory for Vascular Implants, Bioengineering College of Chongqing University, Chongqing, 400030, China.
College of Polymer Science and Engineering, Sichuan University, Chengdu 610065, China.
Theranostics. 2018 Apr 30;8(11):3038-3058. doi: 10.7150/thno.23459. eCollection 2018.
Nanotechnology-based antitumor drug delivery systems, known as nanocarriers, have demonstrated their efficacy in recent years. Typically, the size of the nanocarriers is around 100 nm. It is imperative to achieve an optimum size of these nanocarriers which must be designed uniquely for each type of delivery process. For pH-responsive nanocarriers with programmable size, changes in pH (~6.5 for tumor tissue, ~5.5 for endosomes, and ~5.0 for lysosomes) may serve as an endogenous stimulus improving the safety and therapeutic efficacy of antitumor drugs. This review focuses on current advanced pH-responsive nanocarriers with programmable size changes for anticancer drug delivery. In particular, pH-responsive mechanisms for nanocarrier retention at tumor sites, size reduction for penetrating into tumor parenchyma, escaping from endo/lysosomes, and swelling or disassembly for drug release will be highlighted. Additional trends and challenges of employing these nanocarriers in future clinical applications are also addressed.
基于纳米技术的抗肿瘤药物输送系统，即纳米载体，近年来已证明其疗效。通常，纳米载体的大小约为 100nm。至关重要的是，必须为每种输送过程设计独特的纳米载体的最佳尺寸。对于具有可编程尺寸的 pH 响应纳米载体，pH 值的变化（肿瘤组织约为 6.5，内体约为 5.5，溶酶体约为 5.0）可以作为一种内源性刺激，提高抗肿瘤药物的安全性和疗效。本综述重点介绍了目前用于抗癌药物输送的具有可编程尺寸变化的先进 pH 响应纳米载体。特别是，纳米载体在肿瘤部位的保留、穿透肿瘤实质的尺寸减小、从内体/溶酶体逃逸以及药物释放时的膨胀或解体的 pH 响应机制将被强调。还讨论了在未来临床应用中使用这些纳米载体的其他趋势和挑战。
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