Baicalin functionalized PEI-heparin carbon dots as cancer theranostic agent

The worldwide prevalence of cancer and its significantly rising risks with age have garnered the attention of nanotechnology for prompt detection and effective therapy with minimal or no adverse effects. In the current study, heparin (HP) polymer derived heteroatom (N, S-) co-doped CDs were synthesized using hydrothermal synthesis method to efficiently deliver natural anticancer compound baicalin (BA). Heparin carbon dots (HCDs) were passivated with polyethylenimine (PEI) to improve its fluorescence quantum yield. The surface passivation of CDs by polycationic PEI polymer not only facilitated loading of BA, but also played a crucial role in the pH-responsive drug delivery. The sustained release of BA (up to 80 %) in mildly acidic pH (5.5 and 6.5) conditions endorsed its drug delivery potential for cancer-specific microenvironments. BA-loaded PHCDs exhibited enhanced anticancer activity as compared to BA/PHCDs indicating the effectiveness of the nanoformulation, Furthermore, the flow cytometry analysis confirmed that BA-PHCDs treated cells were arrested in the G2/M phase of cell cycle and had a higher potential for apoptosis. Bioimaging study demonstrated the excellent cell penetration efficiency of PHCDs with complete cytoplasmic localization. All this evidence comprehensively demonstrates the potency of BA-loaded PHCDs as a nanotheranostic agent for cancer.

Automated summary

The study focuses on the synthesis of heparin carbon dots (HCDs) for the efficient delivery of the natural anticancer compound baicalin (BA). The surface passivation of HCDs with polyethylenimine (PEI) improves their fluorescence yield. The sustained release of BA in acidic conditions and enhanced anticancer activity of BA-loaded HCDs demonstrate the potential of this nanotheranostic agent for cancer treatment. Flow cytometry analysis and bioimaging studies confirm the effectiveness of BA-loaded HCDs in arresting cell cycle and penetrating cells.