A novel chemical-based orthogonal bioconjugation strategy to produce tri-functionalized nanoparticles (NPs) an chemotherapy drug, doxorubicin (DOX), a near-infrared cyanine dye (Cy7) and CRGDK homing peptide, a peptide specifically binds to neuropilin-1 (Nrp-1) overexpressed on triple negative breast cancer (TNBC) cells, has been validated. These theranostic NPs have been evaluated in vitro and in vivo using an orthotopic xenotransplant mouse model using TNBC cells. In vitro assays show that theranostic NPs improve the therapeutic index in comparison with free DOX. Remarkably, in vivo studies showed preferred location of theranostic NPs in the tumor area reducing the volume at the same level than free DOX while presenting lower side effects. This multifunctionalized theranostic nanodevice based on orthogonal conjugation strategies could be a good candidate for the treatment and monitoring of Nrp-1 overexpressing tumors. Moreover, this versatile nanodevice can be easily adapted to treat and monitor different cancer types by adapting the conjugation strategy.

中文翻译：

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一种基于正交生物共轭策略的多功能治疗学纳米装置，可有效靶向治疗和监测三阴性乳腺癌。

一种新的基于化学的正交生物共轭策略，可产生三功能纳米颗粒（NPs），化疗药物，阿霉素（DOX），近红外花青染料（Cy7）和CRGDK归巢肽，该肽可特异性结合Neuropilin-1（Nrp -1）在三阴性乳腺癌（TNBC）细胞上过表达，已经得到验证。已使用原位异种移植小鼠模型（使用TNBC细胞）在体外和体内评估了这些治疗性NP。体外测定表明，与游离DOX相比，治疗性NP改善了治疗指数。值得注意的是，体内研究表明，治疗性NPs在肿瘤区域的优选位置与游离DOX相比，在相同水平上减少了体积，同时表现出较低的副作用。这种基于正交共轭策略的多功能治疗学纳米装置可能是治疗和监测Nrp-1过表达肿瘤的良好候选者。而且，这种多功能的纳米装置可通过调整缀合策略而轻松地适用于治疗和监测不同类型的癌症。