目的 以聚乳酸-羥基乙酸共聚物（PLGA）作為納米制劑載體材料將葫蘆素B制備成納米粒，并考察其對HepG2肝癌細(xì)胞的抑制效果。方法 使用乳化溶劑蒸發(fā)法制備葫蘆素B-PLGA載藥納米粒，以PLGA濃度（X₁）、PVA濃度（X₂）和藥物濃度（X₃）作為考察因素，以載藥納米粒的粒徑大小（Y₁）和包封率（Y₂）作為評價(jià)指標(biāo)，應(yīng)用中心復(fù)合設(shè)計(jì)-效應(yīng)面法優(yōu)化葫蘆素B-PLGA載藥納米粒處方；測定了納米粒的粒徑分布和Zeta電位值，通過透射電鏡觀察其微觀形態(tài)，并考察了葫蘆素B-PLGA載藥納米粒的體外藥物釋放特性；比較了葫蘆素B與葫蘆素B-PLGA載藥納米粒對HepG2肝癌細(xì)胞的抑制效果。結(jié)果 葫蘆素B-PLGA載藥納米粒的最優(yōu)處方組成為：PLGA濃度為9.0%，PVA濃度為2.0%，藥物濃度為4.5%，制備的納米粒粒徑為（145.4±15.8） nm，Zeta電位值為（-7.6±0.8） mV；透射電鏡下可觀察到納米粒表面光滑，分布均勻；葫蘆素B-PLGA載藥納米粒釋藥前期出現(xiàn)突釋，后期平緩，48 h藥物釋放達(dá)到86%；葫蘆素B-PLGA載藥納米粒對HepG2肝癌細(xì)胞的抑制作用顯著高于葫蘆素B。結(jié)論 葫蘆素B-PLGA載藥納米?？裳泳徦幬镝尫?，提高對HepG2肝癌細(xì)胞的抑制活性，為進(jìn)一步臨床研究奠定實(shí)驗(yàn)基礎(chǔ)。

Objective To prepare cucurbitacin B-loaded PLGA nanoparticles by using PLGA as carrier material, and to investigate its inhibitory effect on HepG2 liver cancer cells.Methods The cucurbitacin B-loaded PLGA nanoparticles were prepared by emulsion solvent evaporation method. Taking PLGA concentration (X₁), PVA concentration (X₂) and drug concentration (X₃) as the investigation factors, the particle size (Y₁) and encapsulation efficiency (Y₂) of cucurbitacin B-loaded PLGA nanoparticles were used as evaluation indexes. The central composite design-response surface methodology (CCD-RSM) was applied to optimize the formulation of cucurbitacin B-loaded PLGA nanoparticles. The particle size distribution and Zeta potential value were determined. The microscopic morphology was observed by transmission electron microscopy. The in vitro drug release characteristics of cucurbitacin B-loaded PLGA nanoparticles were investigated. The inhibitory effects of cucurbitacin B and cucurbitacin B-loaded PLGA nanoparticles on HepG2 liver cancer cells were compared.Results The optimal formulation of cucurbitacin B-loaded PLGA nanoparticles was:PLGA concentration of 9.0%, PVA concentration of 2.0%, drug concentration of 4.5%. The particle size of (145.4±15.8) nm, and zeta potential of (-7.6±0.8) mV. Transmission electron microscopy showed that the nanoparticles were smooth and uniform in size. The release of cucurbitacin B-loaded PLGA nanoparticles was fast in the early stage, and the late release was slow. Finally, the drug release was 86% within 48 hours. The inhibitory effect of cucurbitacin B-loaded PLGA nanoparticles on HepG2 liver cancer cells was significantly higher than that of cucurbitacin B.Conclusion The cucurbitacin B-loaded PLGA nanoparticles could delay drug release and increase the inhibitory activity of HepG2 liver cancer cells, which lays the experimental foundation for further clinical research.