目的 制备负载阿霉素的黄芩苷纳米粒（DOX/SA-SS-BAI NPs），并评价其体外性能。方法 构建以胱胺为连接臂的海藻酸钠–黄芩苷聚合物，并负载阿霉素，得到DOX/SA-SS-BAI NPs。对DOX/SA-SS-BAI NPs的理化性质进行表征；采用HepG2细胞进行MTT实验验证其细胞毒性。结果 DOX/SA-SS-BAI NPs粒径为（158.2±2.8）nm，PDI为（0.241±0.008），Zeta电位为（−24.1±0.3）mV，包封率为（64.34±0.25）%，载药量为（16.22±0.06）%。体外释放显示载药纳米粒具有良好的还原响应性；MTT实验证明DOX/SA-SS-BAI NPs对HepG2细胞具有良好的抑制作用；细胞摄取实验表明DOX/SA-SS-BAI NPs在HepG2细胞内较快地释放阿霉素。结论 制备的DOX/SA-SS-BAI NPs具有较好的理化性质和体外抗癌作用。

Objective To prepare baicalin nanoparticles loaded with doxorubicin (DOX/SA-SS-BAI NPs), and study in vitro evaluation. Methods Sodium alginate-baicalin copolymer with cystamine as the connecting arm was constructed, and doxorubicin was loaded to obtain DOX/SA-SS-BAI NPs. Physicochemical properties of DOX/SA-SS-BAI NPs were characterized. MTT assay was performed on HepG2 cells to verify cytotoxicity of DOX/SA-SS-BAI NPs. Results The particle size of DOX/SA-SS-BAI NPs was (158.2 ±2.8) nm, PDI was (0.241 ±0.008), Zeta potential was (−24.1 ±0.3) mV, the encapsulation rate was (64.34 ±0.25)%, and the drug load was (16.22 ±0.06)%. In vitro release showed that drug-loaded nanoparticles had good reduction response. MTT assay showed that DOX/SA-SS-BAI NPs had a good inhibitory effect against HepG2 cells. Cell uptake experiments showed that DOX/SA- SS-BAI NPs released doxorubicin rapidly in HepG2 cells. Conclusion Prepared DOX/SA-SS-BAI NPs had good physicochemical properties and in vitro anticancer effect.

R944

河北省自然科学基金-生物医药联合基金培育项目(H2021209024);河北省自然科学基金资助项目(H2018209347)