Jeon H J, Jeong Y I, Jang M K, Park Y H, Nah J W
Department of Polymer Science and Engineering, Sunchon National University, 540-742, Sunchon, South Korea.
Int J Pharm. 2000 Oct 10;207(1-2):99-108. doi: 10.1016/s0378-5173(00)00537-8.
The surfactant-free nanoparticles of poly(DL-lactide-co-glycolide) (PLGA) were prepared by dialysis method without surfactant and physicochemical properties such as particle size and drug contents were investigated against used initial solvent. The size of PLGA nanoparticles and drug contents were significantly changed by used initial solvent. The size of PLGA nanoparticles prepared from dimethylacetamide (DMAc), dimethylformamide (DMF), and dimethylsulfoxide (DMSO) as a initial used solvent was smaller than that of acetone. Selected initial solvent used to dissolve the copolymer significantly affects the size of nanoparticles and drug contents. It was shown that PLGA nanoparticles have spherical shapes from the results of scanning electron microscopy (SEM) and transmission electron microscopy (TEM) observations. It was thought that surfactant-free nanoparticles of PLGA entrapping norfloxacin (NFX) has nice drug loading capacity without free-drug on the surface of nanoparticles through the analysis of X-ray powder diffraction. From these results, it was showed the potential that the PLGA nanoparticles could be formed successively by dialysis method without surfactant. Release kinetics of NFX used as a model drug was governed by not only drug contents but also particle size parameter. The higher the drug contents and the larger the particle size resulted in slower the drug release.
通过透析法在无表面活性剂的情况下制备了聚(DL-丙交酯-共-乙交酯)(PLGA)无表面活性剂纳米颗粒,并针对所使用的初始溶剂研究了其粒度和药物含量等物理化学性质。所使用的初始溶剂显著改变了PLGA纳米颗粒的尺寸和药物含量。以二甲基乙酰胺(DMAc)、二甲基甲酰胺(DMF)和二甲基亚砜(DMSO)作为初始使用溶剂制备的PLGA纳米颗粒的尺寸小于丙酮制备的。用于溶解共聚物的选定初始溶剂显著影响纳米颗粒的尺寸和药物含量。扫描电子显微镜(SEM)和透射电子显微镜(TEM)观察结果表明PLGA纳米颗粒呈球形。通过X射线粉末衍射分析认为,包载诺氟沙星(NFX)的PLGA无表面活性剂纳米颗粒具有良好的载药能力,纳米颗粒表面无游离药物。从这些结果可以看出,通过无表面活性剂的透析法连续形成PLGA纳米颗粒的潜力。用作模型药物的NFX的释放动力学不仅受药物含量的影响,还受粒径参数的影响。药物含量越高,粒径越大,药物释放越慢。