Blood-brain barrier penetrating carbon dots with intrinsic anti-inflammatory and drug-loading properties.

The blood-brain barrier (BBB) is the major obstacle limiting the reach of therapeutic drugs into the brain. Herein, an aspirin-based anti-inflammatory replenisher (aspCD) was fabricated by carbonizing aspirin to deliver drugs into the brain visually. The as-prepared aspCD combined the BBB-penetrating and anti-inflammatory effects of aspirin with the fluorescent and drug-loading properties of carbon dots (CDs), thereby delivering therapeutic drugs into the brain and acting as imaging agent as well as anti-inflammatory replenisher. In vivo experiments of mice and zebrafish revealed that fluorescence aspCD could effectively penetrate BBB. In vitro and in vivo inflammatory models demonstrated that aspCD could be regarded as an excellent anti-inflammatory replenisher. In addition, as a functional carrier, aspCD was proved to be capable of loading drugs with different polarity. In summary, carbonization of active precursors (therapeutic drugs) into CDs could be a promising strategy to achieve the loading and visualization of drugs as well as the retainment of their biological activities.