The improvement of the pharmacological profile of lipophilic drug formulations is one of the main successes achieved using nanoparticles (NPs) in medicine. However, the complex synthesis procedure and numerous post-processing steps hamper the cost-effective use of these formulations. In this work, an approach which requires only a syringe to produce self-assembling biodegradable and biocompatible poly(caprolactone)-based NPs is developed. The effective synthesis of monodisperse NPs has been made possible by the optimization of the block-copolymer synthesized via a combination of ring opening polymerization and reversible addition-fragmentation chain transfer polymerization. These NPs can be used to formulate lipophilic drugs that are barely soluble in water, such as trabectedin, a potent anticancer therapeutic. Its biodistribution and antitumor activity have been compared with the commercially available formulation Yondelis®. The results indicate that this trabectedin NP formulation performs with the same antitumor activity as Yondelis®, but does not have the drawback of severe local vascular toxicity in the injection site.

亲脂性药物制剂的药理作用的改善是在医学中使用纳米颗粒（NPs）取得的主要成功之一。但是，复杂的合成过程和大量的后处理步骤阻碍了这些制剂的成本有效使用。在这项工作中，开发了一种仅需要注射器即可生产自组装可生物降解和生物相容性聚己内酯基NP的方法。通过优化开环聚合反应和可逆加成-断裂链转移聚合反应合成的嵌段共聚物，可以有效地合成单分散NP。这些NP可用于配制几乎不溶于水的亲脂性药物，例如trabectedin（一种有效的抗癌治疗剂）。已将其生物分布和抗肿瘤活性与市售制剂进行了比较。结果表明该trabectedin NP制剂具有与Yondelis®相同的抗肿瘤活性，但在注射部位没有严重的局部血管毒性的缺点。