负载阿霉素的黄芩苷纳米粒的制备及其体外性能评价

Preparation and in vitro evaluation of baicalin nanoparticles loaded with doxorubicin

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.