槲皮素聚氰基丙烯酸正丁酯纳米粒子的制备、表征和体外抗人子宫内膜癌作用

Preparation and characterization of Quercetin Polybutylcyanoacrylate Nanoparticles and its anti-human endometrial cancer in vitro

目的制备槲皮素聚氰基丙烯酸正丁酯纳米粒子(QT-PBCA)并考察其理化性质、体外抗人子宫内膜癌作用。方法采用阴离子乳液聚合法制备QT-PBCA纳米粒子。透射电镜观察纳米粒子的形态,Zeta电位仪检测粒径和Zeta电位,红外光谱仪检测QT-PBCA纳米粒子、BCA单体、QT、空载体PBCA纳米粒子的红外吸收光谱,MTT法检测细胞存活率。结果QT-PBCA纳米粒子呈球形或椭圆形,表面光滑,在透射电镜下因PBCA固有的黏合特性而处于略微聚集的状态,其平均粒径为(161.1±0.44)nm,Zeta电位为(-7.28±0.60)mV,平均包封率为(79.86±0.45)%。在纳米粒子的封装以及制备的过程中槲皮素与聚合物之间可能发生的反应。槲皮素封存到PBCA纳米粒子中是靠分子间作用力(如氢键)完成的。随着顺铂、纳米粒子浓度的增加,JEC、LO2细胞的存活率降低,且顺铂组相比于纳米粒子组的存活率要更低(P<0.05)。纳米粒子在6.67 mg/L对LO2细胞有一定的毒性,但随着浓度增高,反而会产生促进细胞增殖的作用。结论 QT-PBCA纳米粒子具有良好的理化性质和抗肿瘤作用且对正常细胞无害,有潜力成为新型抗癌药物。

Objective To prepare Quercetin Polybutylcyanoacrylate(QT-PBCA)Nanoparticles and study its physicochemical properties and anti-human endometrial cancer effect in vitro.Methods QT-PBCA nanoparticles were prepared by anionic emulsion polymerization method.Morphology of the nanoparticles was observed with transmission electron microscopy.Particle size and Zeta potential were detected with Zeta potentiometer.IR of QT-PBCA nanoparticles,BCA monomers,QT,and empty carrier PBCA nanoparticles were measured with infrared spectrometer.Cell proliferation rate was measured by MTT method.Results The prepared QT-PBCA nanoparticles were spherical or elliptical,indicating that they were smooth.They were slightly aggregated under the transmission electron microscope due to the inherent adhesion characteristics of PBCA.The average particle diameter was(161.1±0.44)nm,and the Zeta potential was(-7.28±0.60)mV,and the average encapsulation rate was(79.86±0.45)%.The possible reaction between quercetin and polymer happened during the encapsulation and preparation of nanoparticles.Quercetin was encapsulated into PBCA nanoparticles by intermolecular forces,such as hydrogen bonds.After the treatment of JEC and LO2 cells with different concentrations of cisplatin and QT-PBCA nanoparticles,the survival rate of JEC and LO2 cells decreased with the increase of cisplatin concentration,and the survival rate was lower than that of the treatment group(P<0.05).QT-PBCA nanoparticles had certain toxicity to LO2 cells at a concentration of 6.67 mg/L,but as the concentration increased,they could instead promote cell proliferation.Conclusion QT-PBCA nanoparticles have good physical and chemical properties,anti-tumor effects,and are not harmful to normal cells.They have the potential to become new anticancer drugs.