The ability to produce nanotherapeutics at large‐scale with high drug loading efficiency, high drug loading capacity, high stability, and high potency is critical for clinical translation. However, many nanoparticle‐based therapeutics under investigation suffer from complicated synthesis, poor reproducibility, low stability, and high cost. In this work, a simple method for preparing multifunctional nanoparticles is utilized that act as both a contrast agent for magnetic resonance imaging and a photosensitizer for photodynamic therapy for the treatment of cancer. In particular, the photosensitizer protoporphyrin IX (PpIX) is used to solubilize small nanoclusters of superparamagnetic iron oxide nanoparticles (SPIONs) without the use of any additional carrier materials. These nanoclusters are characterized with a high PpIX loading efficiency; a high loading capacity, stable behavior; high potency; and a synthetic approach that is amenable to large‐scale production. In vivo studies of photodynamic therapy (PDT) efficacy show that the PpIX‐coated SPION nanoclusters lead to a significant reduction in the growth rate of tumors in a syngeneic murine tumor model compared to both free PpIX and PpIX‐loaded poly(ethylene glycol)‐polycaprolactone micelles, even when injected at 1/8th the dose. These results suggest that the nanoclusters developed in this work can be a promising nanotherapeutic for clinical translation.

中文翻译：

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原卟啉 IX (PpIX) 涂层超顺磁性氧化铁纳米颗粒 (SPION) 纳米团簇用于磁共振成像和光动力治疗

大规模生产高载药效率、高载药量、高稳定性和高效力的纳米药物的能力对于临床转化至关重要。然而，许多正在研究的基于纳米颗粒的疗法存在合成复杂、重现性差、稳定性低和成本高等问题。在这项工作中，采用了一种制备多功能纳米颗粒的简单方法，该纳米颗粒既可作为磁共振成像的造影剂，又可作为癌症光动力疗法的光敏剂。特别是，光敏剂原卟啉 IX (PpIX) 用于溶解超顺磁性氧化铁纳米颗粒 (SPION) 的小纳米团簇，无需使用任何额外的载体材料。这些纳米团簇具有高 PpIX 负载效率；负载能力高，行为稳定；高效力；以及适合大规模生产的合成方法。光动力疗法（PDT）功效的体内研究表明，与游离 PpIX 和负载 PpIX 的聚（乙二醇）相比，PpIX 涂覆的 SPION 纳米团簇导致同基因小鼠肿瘤模型中肿瘤的生长速率显着降低。聚己内酯胶束，即使以 1/8 剂量注射时也是如此。这些结果表明，这项工作中开发的纳米簇可以成为临床转化的有前途的纳米治疗药物。