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Preparation and release characteristics of insulin and insulin-like growth factor-one from polymer nanoparticles

机译:高分子纳米颗粒制备胰岛素和类胰岛素生长因子一的特性

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Two methods of preparing polymer nanoparticles containing (a) insulin and (b) insulin-like growth factor-1 were compared and the influence of process parameters on size and release characteristics was determined.Poly(lactide-glycolide)co-polymer (50:50) was used in both methods.Method one used a salting-out process;while method two used a solvent evaporation/double emulsion procedure forming a w/o/w secondary emulsion.Particles were separated by centrifugation and dried under vacuum.Particle size was analysed by scanning electron microscopy and protein release by dissolution and high pressure liquid chromatography.Method one produced particles of diameter 0.3-0.8 mu m,whereas method two gave larger particles of 0.76-1.05 mu m and in both procedures reducing pH also decreased particle size.Optimal emulsifying speed was below 4000 rpm and scanning electron micrographs showed smooth spherical particles.Release characteristics of insulin and IGF-1 in method one and two were similar releasing 60% in 10 days but in method one release was diminished to 8% over a similar time period.Method one proved successful in producing spheres of the required size range but hampered protein loading by denaturation resulting in a low release rate.Method two provided an acceptable release rate but produced particles with diameters of about one micron.
机译:比较了两种制备包含(a)胰岛素和(b)胰岛素样生长因子-1的聚合物纳米颗粒的方法,并确定了工艺参数对尺寸和释放特性的影响。聚(丙交酯-乙交酯)共聚物(50:两种方法均使用50),方法一采用盐析法,而方法二采用溶剂蒸发/双乳化程序形成w / o / w二次乳化液,离心分离颗粒并真空干燥,粒径为方法一产生直径为0.3-0.8微米的颗粒,而方法二产生直径为0.76-1.05微米的较大颗粒,在两种方法中降低pH值也减小了粒径最佳乳化速度在4000 rpm以下,扫描电子显微镜照片显示光滑的球形颗粒。方法1和2中胰岛素和IGF-1的释放特性相似在10天内达到60%,但在方法1中的释放在相似的时间段内减少至8%。方法1被证明可成功生产所需大小范围的球体,但由于变性而阻碍了蛋白质的装载,从而导致较低的释放率。方法2可接受的释放速率,但产生的颗粒直径约为1微米。

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