Tumor Precision Targeting Research Center, School of Environmental and Chemical Engineering, Shanghai University, Shanghai, 200444, P. R. China.
Institute of Biophysics, Chinese Academy of Sciences, Beijing, 100101, P. R. China.
Adv Mater. 2019 Oct;31(40):e1902409. doi: 10.1002/adma.201902409. Epub 2019 Aug 1.
Advantages such as strong signal strength, resistance to photobleaching, tunable fluorescence emissions, high sensitivity, and biocompatibility are the driving forces for the application of fluorescent nanoparticles (FNPs) in cancer diagnosis and therapy. In addition, the large surface area and easy modification of FNPs provide a platform for the design of multifunctional nanoparticles (MFNPs) for tumor targeting, diagnosis, and treatment. In order to obtain better targeting and therapeutic effects, it is necessary to understand the properties and targeting mechanisms of FNPs, which are the foundation and play a key role in the targeting design of nanoparticles (NPs). Widely accepted and applied targeting mechanisms such as enhanced permeability and retention (EPR) effect, active targeting, and tumor microenvironment (TME) targeting are summarized here. Additionally, a freshly discovered targeting mechanism is introduced, termed cell membrane permeability targeting (CMPT), which improves the tumor-targeting rate from less than 5% of the EPR effect to more than 50%. A new design strategy is also summarized, which is promising for future clinical targeting NPs/nanomedicines design. The targeting mechanism and design strategy will inspire new insights and thoughts on targeting design and will speed up precision medicine and contribute to cancer therapy and early diagnosis.
荧光纳米粒子（FNPs）在癌症诊断和治疗中的应用得益于其诸多优势，如信号强度强、抗光漂白、荧光发射可调谐、灵敏度高、生物相容性好等。此外，FNPs 的大表面积和易于修饰为用于肿瘤靶向、诊断和治疗的多功能纳米粒子（MFNPs）的设计提供了一个平台。为了获得更好的靶向和治疗效果，有必要了解 FNPs 的特性和靶向机制，这是靶向设计的基础，在纳米粒子（NPs）的靶向设计中起着关键作用。本文总结了广泛接受和应用的靶向机制，如增强的通透性和保留（EPR）效应、主动靶向和肿瘤微环境（TME）靶向。此外，还介绍了一种新发现的靶向机制，称为细胞膜通透性靶向（CMPT），它将肿瘤靶向率从 EPR 效应的不到 5%提高到了 50%以上。还总结了一种新的设计策略，这对未来临床靶向 NPs/纳米药物设计具有广阔的前景。该靶向机制和设计策略将为靶向设计带来新的见解和思路，并将加速精准医学的发展，为癌症治疗和早期诊断做出贡献。
