Department of Pharmaceutics, School of Pharmaceutical Sciences, Shandong University, Ji'nan, PR China.
Curr Pharm Des. 2012;18(23):3442-51. doi: 10.2174/138161212801227122.
Polymeric micelles (PMs) belong to supramolecular core-shell-type assemblies. PMs are from amphiphilic block copolymers with several tens of nanometers in diameter. An important criterion verifying the effectiveness of micellar drug carriers is the ability to control the location and time over which drug release occurs. The pH variations in the body are particularly important in the development of micellar carriers for treating diseases such as cancer and inflammation. pH-sensitive PMs have emerged as a fascinating class of nanoscopic drug carriers that can be elegantly applied for programmed drug and gene delivery. In this review, we provide an analysis of recent literature reports on these pH-sensitive PMs. Different approaches that have been taken to develop pH-sensitive PMs are highlighted, including incorporating pH-sensitive building blocks such as poly(L-histidine) and poly(β-amino ester), and acid degradable linkages such as hydrazones and acetals. The potential applications of pH-sensitive PMs within the biomedical field are also summarized.
聚合物胶束(PMs)属于超分子核壳型组装体。PMs 由几十纳米直径的两亲性嵌段共聚物组成。验证胶束药物载体有效性的一个重要标准是控制药物释放发生的位置和时间的能力。在开发用于治疗癌症和炎症等疾病的胶束载体时,体内的 pH 值变化尤为重要。pH 敏感 PMs 已成为一类引人注目的纳米级药物载体,可以巧妙地应用于程序性药物和基因传递。在这篇综述中,我们分析了最近关于这些 pH 敏感 PMs 的文献报道。强调了开发 pH 敏感 PMs 的不同方法,包括引入 pH 敏感结构单元,如聚(L-组氨酸)和聚(β-氨基酯),以及酸可降解键,如腙键和缩醛键。还总结了 pH 敏感 PMs 在生物医学领域的潜在应用。