Accumulating evidence suggests that the flavone glycoside baicalin has immunomodulatory effects and antitumor potential. However, its weak stability in solution, poor absorption, and low bioavailability limit its clinical application. To overcome these disadvantages, we developed baicalin-loaded poly(lactic-co-glycolic acid) nanoparticles (PLGA-B) of small size. Next, we evaluated the dual function of immunotherapy and chemotherapy for PLGA-B using immune-related cells and tumor cells. Results showed that PLGA-B were spherical, with a particle size ∼120 nm and narrow size distribution with an excellent polydispersity index of 0.103. In vitro experiments revealed that baicalin and PLGA-B could activate dendritic cells (DCs) to have higher expression of surface marker molecules and costimulatory molecules than those of control cells. Baicalin and PLGA-B could trigger apoptosis in melanoma (B16) cells via cell-cycle arrest at the G2/M phase. These data suggest that PLGA-B have important roles in activating DCs and killing melanoma cells. Our study could lay a foundation for melanoma treatment through a combined strategy of immunotherapy and chemotherapy.

越来越多的证据表明，黄酮苷黄ical苷具有免疫调节作用和抗肿瘤潜力。然而，其在溶液中的弱稳定性，吸收差和生物利用度低限制了其临床应用。为了克服这些缺点，我们开发了黄芩加载聚（乳酸-共-乙醇酸）小尺寸的纳米粒子（PLGA-B）。接下来，我们使用免疫相关细胞和肿瘤细胞评估了PLGA-B免疫疗法和化学疗法的双重功能。结果显示PLGA-B为球形，粒径约120 nm，粒径分布窄，多分散指数为0.103。体外实验表明，黄ical苷和PLGA-B可以激活树突状细胞（DC），使其表面标记分子和共刺激分子的表达高于对照细胞。黄ical苷和PLGA-B可以通过G2 / M期细胞周期停滞来触发黑色素瘤（B16）细胞凋亡。这些数据表明，PLGA-B在激活DC和杀死黑色素瘤细胞方面具有重要作用。我们的研究可以通过结合免疫疗法和化学疗法为黑色素瘤治疗奠定基础。