Nucleolus‐Targeted Photodynamic Anticancer Therapy Using Renal‐Clearable Carbon Dots

Abstract

Photodynamic therapy (PDT), which utilizes light excited photosensitizers (PSs) to generate reactive oxygen species (ROS) and consequently ablate cancer cells or diseased tissue, has attracted a great deal of attention in the last decades due to its unique advantages. In order to further enhance PDT effect, PSs are functionalized to target specific sub‐cellular organelles, but most PSs cannot target nucleolus, which is demonstrated as a more efficient and ideal site for cancer treatment. Here, an effective carbon dots (C‐dots) photosensitizer with intrinsic nucleolus‐targeting capability, for the first time, is synthesized, characterized, and employed for in vitro and in vivo image‐guided photodynamic anticancer therapy with enhanced treatment performance at a low dose of PS and light irradiation. The C‐dots possess high ROS generation efficiency and fluorescence quantum yield, excellent in vitro and in vivo biocompatibility, and rapid renal clearance, endowing it with a great potential for future translational research.

In Vivo Biodistribution, Clearance, and Biocompatibility of Multiple Carbon Dots Containing Nanoparticles for Biomedical Application

“…It has been reported that glomerular filtration by the kidneys is highly size-selective [40,41]. Previous in vivo biodistribution studies of single carbon dots with a diameter less than 10 nm proved that the kidneys were the main clearance organ [42][43][44]. Our results indicate that the CDs@PEI nanoparticles with approximately 100 nm in diameter could be excreted from the intestine in the feces.…”

Two-photon excitable membrane targeting polyphenolic carbon dots for long-term imaging and pH-responsive chemotherapeutic drug delivery for synergistic tumor therapy

“…4 Various chemotherapeutic drugs, such as cisplatin (CDDP), paclitaxel (PTX), doxorubicin (Dox), and camptothecin (CPT), are often conjugated with drug delivery vehicles (DDVs) for targeted delivery to the nucleus of tumor cells. [5][6][7] Dox (an anthracycline drug) interacts with DNA via electrostatic interaction, resulting in DNA synthesis inhibition and apoptotic cell death. 8,9 Unlike traditional DDVs, which are mostly associated with cytoplasmic delivery, nuclear-targeted DDVs are highly effective owing to their superior ability to deliver drugs into the nucleus.…”

Recent progress of carbon dots in targeted bioimaging and cancer therapy

“…Therefore, the scope of PDT treatment with CDs can be extended from tumor treatment to other application fields, such as antibacterial treatment, wound healing, inflammatory treatment, plant preservation and so on. For example, Pang et al designed one kind of CDs with both intrinsic nucleolus-targeting and ROS generation capability (Figure 14 A) 224 . With more efficient tumor treatment induced by the ROS located within nucleolus and nucleolus from the CDs, the enhanced in vitro and in vivo PDT at a low dose of CDs and light irradiation were achieved.…”