癌症的全球发病率以及其随年龄增长而显著升高的风险，已引起纳米技术的关注，以便能够快速检测和有效治疗癌症，并且最小化或不产生不良影响。在本研究中，利用水热合成方法合成了以肝素（HP）聚合物为基础，杂原子（N，S-）共掺杂的碳点（CDs），用于高效递送天然抗癌化合物黄芩苷（BA）。为了提高其荧光量子产率，肝素碳点（HCDs）经过聚乙烯亚胺（PEI）保护。通过阳离子性聚乙烯亚胺聚合物对碳点进行表面离子给药，不仅促进了黄芩苷的负载，而且在pH响应型药物释放中起着关键作用。在微弱酸性pH（5.5和6.5）条件下，黄芩苷的持续释放（高达80%）证明了其对特定癌症微环境的潜在药物释放能力。相较于单独黄芩苷的药物，负载黄芩苷的肝素碳点显示出更强的抗癌活性，表明了该纳米制剂的有效性。此外，流式细胞仪分析证实，黄芩苷-肝素碳点处理的细胞停留在细胞周期的G2/M期，具有更高的凋亡潜力。生物成像研究显示了肝素碳点在细胞穿透效率方面的优异性，且完全定位于细胞质。所有这些证据全面地证明了负载黄芩苷的肝素碳点作为一种用于癌症的纳米诊疗剂的潜力。版权©2023 Elsevier B.V. 保留所有权利。

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.Copyright © 2023 Elsevier B.V. All rights reserved.