School of Chemistry , University of Birmingham , Edgbaston, Birmingham , B15 2TT , United Kingdom.
Department of Chemistry , The University of Warwick , Gibbet Hill Road , Coventry CV4 7AL , United Kingdom.
Biomacromolecules. 2018 Aug 13;19(8):3427-3434. doi: 10.1021/acs.biomac.8b00744. Epub 2018 Jul 6.
Polymeric nanoparticles are widely investigated to enhance the selectivity of therapeutics to targeted sites, as well as to increase circulation lifetime and water solubility of poorly soluble drugs. In contrast to the encapsulation of the cargo into the nanostructures, the conjugation directly to the polymer backbone allows better control on the loading and selective triggered release. In this work we report a simple procedure to create biodegradable polycarbonate graft copolymer nanoparticles via a ring opening polymerization and subsequent postpolymerization modification strategies. The polymer, designed with both pH-responsive acetal linkages and a norbornene group, allows for highly efficient postpolymerization modifications through a range of chemistries to conjugate imaging agents and solubilizing arms to direct self-assembly. To demonstrate the potential of this approach, polycarbonate-based nanoparticles were tested for biocompatibility and their ability to be internalized in A549 and IMR-90 cell lines.
高分子纳米粒子被广泛研究用于提高治疗剂对靶向部位的选择性，以及增加水溶性差的药物的循环半衰期。与将货物包封在纳米结构内相比，直接将药物连接到聚合物主链上可以更好地控制载药量和选择性触发释放。在这项工作中，我们报告了一种通过开环聚合和随后的后聚合修饰策略来制备可生物降解的聚碳酸酯接枝共聚物纳米粒子的简单方法。该聚合物设计有 pH 响应性缩醛键和降冰片烯基团，允许通过一系列化学反应进行高效的后聚合修饰，以将成像剂和增溶臂连接到聚合物上，从而实现自组装。为了证明这种方法的潜力，我们测试了基于聚碳酸酯的纳米粒子的生物相容性及其在 A549 和 IMR-90 细胞系中内化的能力。
