National Traditional Chinese Medicine Clinical Research Base, Affiliated Traditional Chinese Medicine Hospital, Southwest Medical University, Luzhou, 646000, China.
Beijing National Laboratory for Molecular Sciences, CAS Research/Education Center for Excellence in Molecular Sciences, Key Laboratory of Analytical Chemistry for Living Biosystems, Beijing, 100190, China.
ChemMedChem. 2021 Feb 17;16(4):646-653. doi: 10.1002/cmdc.202000420. Epub 2020 Oct 28.
Negatively charged fluorescent carbon dots (CDs, E =608 nm) were hydrothermally prepared from thiophene phenylpropionic acid polymers and then successfully loaded with the positively charged anticancer cargo coptisine, which suffers from poor bioavailability. The formed CD-coptisine complexes were thoroughly characterized by particle size, morphology, drug loading efficiency, drug release, cellular uptake and cellular toxicity in vitro and antitumor activities in vivo. In this nano-carrier system, red emissive CDs possess multiple advantages as follows: 1) high drug loading efficiency (>96 %); 2) sustained drug release; 3) enhanced drug efficacy towards cancer cells; 4) EPR effect; 5) drug release tracing with near-infrared imaging. These properties indicated that red emissive CDs prepared from polymers could be used as a novel drug delivery system with integrated therapeutic and imaging functions in cancer therapy, which are expected to have great potential in future clinical applications.
负电荷荧光碳点(CDs,E = 608nm)由噻吩苯丙酸聚合物水热制备,然后成功负载带正电荷的抗癌药物黄连碱,黄连碱的生物利用度较差。所形成的 CD-黄连碱复合物通过粒径、形态、药物装载效率、药物释放、细胞摄取和细胞毒性进行了全面的体外表征和体内抗肿瘤活性。在这个纳米载体系统中,红色发光 CD 具有以下多个优点:1)高药物装载效率(>96%);2)持续的药物释放;3)增强对癌细胞的药物疗效;4)EPR 效应;5)近红外成像的药物释放追踪。这些特性表明,由聚合物制备的红色发光 CDs 可用作具有综合治疗和成像功能的新型药物传递系统,有望在未来的临床应用中具有巨大的潜力。