[关键词]
[摘要]
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。
[Key word]
[Abstract]
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.
[中图分类号]
R944
[基金项目]
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)