载汉防己甲素PLGA磁性纳米粒的制备分离及理化性质研究

目的:制备复合型核-壳磁性纳米粒,将其与药物汉防己甲素共同包载于聚乳酸-羟基乙酸共聚物(PLGA)中,运用磁珠分选(MACS)技术分离纯化载药PLGA磁性纳米粒,研究其理化性质及药物包封率。方法:采用钴铁纳米颗粒的合成及核壳结构的生长两步法制备CoFe₂O₄ NPs@MnFe₂O₄纳米粒,采用乳化分散法制备载汉防己甲素PLGA磁性纳米粒;采用MACS技术分离未被包载的药物及无磁性的PLGA纳米粒;利用激光粒径仪DLS、扫描电镜SEM、透射电镜TEM、振动样品磁强计VSM对纳米粒的理化性质及磁性能进行考察;采用RP-HPLC法测定药物载药量、包封率。结果:经MACS磁分离的载汉防己甲素PLGA磁性纳米粒平均粒径195.9 nm,其中CoFe₂O₄ NPs@MnFe₂O₄纳米粒为13.6 nm;载药PLGA磁性纳米粒呈表面光滑圆球形,磁性材料均匀分散在纳米粒内部;VSM结果显示载汉防己甲素磁性PLGA纳米粒具有良好的超顺磁性;RP-HPLC法测定载汉防己甲素磁性PLGA纳米粒包封率和载药量分别为(60.57±2.81)%及(1.83±0.27)%。结论:采用MACS分离纯化的载汉防己甲素PLGA磁纳米粒大小均一,具超顺磁性,有较高的包封率和载药量,有进一步研究的价值。

Objective: To prepare the complex core-shell magnetic nanoparticles, and entrap them into the polylacticglycolidc acidcopolymer(PLGA) with tetrandrine;to purify the co-loaded PLGA nanoparticles by MACS separation technique and further investigate the physicochemical characters and the drug-loading property. Methods: The CoFe₂O₄ NPs@MnFe₂O₄ nanoparticles were prepared by the cobalt iron synthesis and the twostep growth process of core-shell structure, while the co-loaded PLGA NPs were prepared by the emulsion solvent diffusion method.The MACS method was used to separate the free drug and blank PLGA nanoparticles.The physicochemical and magnetic characters of co-loaded PLGA NPs were investigated by DLS, SEM, TEM and VSM.The RP-HPLC analysis was used to measure the drug loading and the entrapment efficiency.Results: The mean size of tetrandrine loaded PLGA magnetic nanoparticles after being purified by the MACS column was 195.9 nm, and the diameter of CoFe₂O₄ NPs@MnFe₂O₄ was around 13.6 nm.The co-loaded PLGA NPs showed spherical shape with smooth surface and the CoFe₂O₄ NPs@MnFe₂O₄ NPs were homogeneously distributed inside the polymeric nanoparticles.The VSM result indicated that the co-loaded PLGA NPs were superparamagnetic. The drug loading and the entrapment efficiency were(1.83±0.27)% and (60.57±2.81)% by RP-HPLC measurement.Conclusion: Tet-PLGA magnetic NPs showed uniform particle size, superparamagnetic property, good entrapment efficiency and drug loading.Due to these advantages, the co-loaded PLGA NPs is worth further study.