目的 制備負載阿霉素的黃芩苷納米粒（DOX/SA-SS-BAI NPs），并評價其體外性能。方法 構建以胱胺為連接臂的海藻酸鈉–黃芩苷聚合物，并負載阿霉素，得到DOX/SA-SS-BAI NPs。對DOX/SA-SS-BAI NPs的理化性質進行表征；采用HepG2細胞進行MTT實驗驗證其細胞毒性。結果 DOX/SA-SS-BAI NPs粒徑為（158.2±2.8）nm，PDI為（0.241±0.008），Zeta電位為（−24.1±0.3）mV，包封率為（64.34±0.25）%，載藥量為（16.22±0.06）%。體外釋放顯示載藥納米粒具有良好的還原響應性；MTT實驗證明DOX/SA-SS-BAI NPs對HepG2細胞具有良好的抑制作用；細胞攝取實驗表明DOX/SA-SS-BAI NPs在HepG2細胞內(nèi)較快地釋放阿霉素。結論 制備的DOX/SA-SS-BAI NPs具有較好的理化性質和體外抗癌作用。

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

河北省自然科學基金-生物醫(yī)藥聯(lián)合基金培育項目(H2021209024);河北省自然科學基金資助項目(H2018209347)