State Key Laboratory of Natural Medicines, Jiangsu Key Laboratory of Carcinogenesis and Intervention, China Pharmaceutical University, Nanjing, 210009, P. R. China.
Department of Chemistry and Biochemistry, Florida International University, Miami, FL, USA.
J Mater Chem B. 2020 Mar 11;8(10):2040-2047. doi: 10.1039/c9tb01818b.
Squamous cell carcinoma (SCC) is a usually responds poorly to treatment suffers from poor therapeutic benefits while oroxylin A (OA) is a promising flavonoid with high anticancer efficacy against various cancer types. Here in our study, in order to reveal the potential of OA based drug delivery systems (DDSs) in the treatment of SCC, we firstly revealed that OA had a certain pharmacodynamic effect on skin SCC (A431 cells). Afterwards, OA was loaded into a newly synthesized aggregation-induced emission (AIE)-active polymer to construct OA-loaded PDots for the first time. Our results revealed that OA-loaded PDots showed preferable drug loading and enhanced stability. Moreover, the DDS was also capable of self-illumination in the aggregate state to reveal the uptake profile. Most importantly, the DDS showed much more elevated anticancer benefits than free OA in vitro and advanced tumor targetability in vivo, suggesting that it might be a promising system against SCC.
鳞状细胞癌 (SCC) 通常对治疗反应不佳，治疗效果不佳，而白杨素 A (OA) 是一种很有前途的黄酮类化合物，对多种癌症类型具有高抗癌功效。在我们的研究中，为了揭示基于 OA 的药物递送系统 (DDS) 在 SCC 治疗中的潜力，我们首先揭示 OA 对皮肤 SCC(A431 细胞)具有一定的药效。随后，OA 被载入一种新合成的聚集诱导发射 (AIE) 活性聚合物中，首次构建了负载 OA 的 PDots。我们的结果表明，负载 OA 的 PDots 表现出更好的药物负载和增强的稳定性。此外，该 DDS 在聚集状态下也能够自发光，从而揭示摄取情况。最重要的是，该 DDS 在体外表现出比游离 OA 更高的抗癌功效，并且在体内具有更高的肿瘤靶向性，表明它可能是一种有前途的 SCC 治疗系统。
