State Key Laboratory of Electroanalytical Chemistry, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun 130022, China.
University of Chinese Academy of Sciences, Beijing 100049, China.
Theranostics. 2017 Oct 17;7(19):4689-4698. doi: 10.7150/thno.21672. eCollection 2017.
Biodegradable polymeric nanomaterials can be directly broken down by intracellular processes, offering a desirable way to solve toxicity issues for cancer diagnosis and treatment. Among them, aliphatic polycarbonates are approved for application in biological fields by the United States Food and Drug Administration (FDA), however, high hydrophobicity, deficient functionality and improper degradation offer significant room for improvement in these materials.
To achieve progress in this direction, herein, we demonstrate that CO-based amphiphilic polycarbonates (APC) with improved hydrophilicity and processability can be used as a reliable and efficient platform for tumor imaging. To better investigate their potential, we devised a convenient strategy through conjugation of APC with gadolinium (Gd).
The resulting polymeric micelles (APC-DTPA/Gd) exhibit excellent magnetic resonance imaging performance, simultaneously enabling real-time visualization of bioaccumulation and decomposition of polymeric micelles . Importantly, these micelles can be degraded to renally cleared products within a reasonable timescale without evidence of toxicity.
Our findings may help the development of CO-based amphiphilic polycarbonate for cancer diagnosis and treatment, accompanied by their low-toxicity degradation pathway.
可生物降解的聚合纳米材料可以被细胞内过程直接分解，为解决癌症诊断和治疗的毒性问题提供了一种理想的方法。其中，脂肪族聚碳酸酯已被美国食品和药物管理局（FDA）批准应用于生物领域，然而，其高疏水性、功能不足和不当降解为这些材料的改进提供了很大的空间。
为了在这一方向取得进展，本文展示了具有改善的亲水性和可加工性的基于 CO 的两亲性聚碳酸酯（APC）可用作肿瘤成像的可靠高效平台。为了更好地研究其潜力，我们通过 APC 与钆（Gd）的缀合设计了一种方便的策略。
所得的聚合物胶束（APC-DTPA/Gd）表现出优异的磁共振成像性能，同时能够实时可视化聚合物胶束的生物积累和分解。重要的是，这些胶束可以在合理的时间内降解为可经肾脏清除的产物，而没有毒性的证据。
我们的发现可能有助于开发用于癌症诊断和治疗的基于 CO 的两亲性聚碳酸酯，并伴随其低毒性的降解途径。
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