Chae Ji-Man, Mo Sei-Myoung, Oh In-Joon
College of Pharmacy and Research Institute of Drug Development, Chonnam National University, Gwangju 500-757, Korea.
J Nanosci Nanotechnol. 2010 May;10(5):3224-7. doi: 10.1166/jnn.2010.2242.
We tested the effects of poloxamer 188 on the preparation and characteristics of poly(lactice-co-glycolide) (PLGA) nanoparticles containing all-trans retinoic acid (ATRA). Spherical nanoparticles incorporated ATRA were prepared by an emulsification-diffusion method increasing concentrations of poloxamer 188 decreased nanoparticle size. The endothermic peak of ATRA at 183 degrees C disappeared in the nanoparticles and X-ray diffraction measurements showed the disappearance of characteristics of ATRA suggesting the change of the crystallinity of ATRA in the nanoparticles to an amorphous state. ATRA release in vitro increased as the concentration of poloxamer increased. The mean residence time of ATRA-loaded nanoparticles after the administration of a single intravenous dose to rats was longer than that of the sodium ATRA solution. The anti-cancer activity of ATRA-loaded nanoparticles in the human leukemia-60 cell line was similar to free ATRA. Thus, PLGA/poloxamer nanoparticles can provide a sustained release preparation of ATRA.
我们测试了泊洛沙姆188对含全反式维甲酸（ATRA）的聚（丙交酯-乙交酯）（PLGA）纳米颗粒的制备及特性的影响。通过乳化-扩散法制备了包载ATRA的球形纳米颗粒，增加泊洛沙姆188的浓度会使纳米颗粒尺寸减小。纳米颗粒中ATRA在183℃的吸热峰消失，X射线衍射测量显示ATRA的特征消失，这表明纳米颗粒中ATRA的结晶度转变为非晶态。体外ATRA释放随泊洛沙姆浓度增加而增加。对大鼠单次静脉注射给药后，载ATRA纳米颗粒的平均驻留时间比ATRA钠溶液的长。载ATRA纳米颗粒在人白血病-60细胞系中的抗癌活性与游离ATRA相似。因此，PLGA/泊洛沙姆纳米颗粒可提供ATRA的缓释制剂。
