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聚合物衍生的红色发光碳点作为高效纳米载体用于黄连碱体内和体外递送。

Red Emissive Carbon Dots Prepared from Polymers as an Efficient Nanocarrier for Coptisine Delivery in vivo and in vitro.

机构信息

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.

出版信息

ChemMedChem. 2021 Feb 17;16(4):646-653. doi: 10.1002/cmdc.202000420. Epub 2020 Oct 28.

DOI:10.1002/cmdc.202000420
PMID:32959534
Abstract

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.

摘要

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。

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