成骨生长肽壳聚糖—海藻酸钠微球的制备及体外检测

背景:成骨生长肽体外注射可以刺激外周血和骨髓细胞数增加,增加动物的骨量,加速骨折愈合,但因多肽不稳定性及注射应用不方便,限制了其临床应用。目的:应用乳化交联法制备成骨生长肽壳聚糖-海藻酸钠缓释微球,并对其粒径、载药、体外释药、理化特性进行检测。方法:以戊二醛作为交联剂,应用乳化交联法制备具有控制释放功能的负载成骨生长肽壳聚糖-海藻酸钠微球,显微镜及扫描电镜观察微球的形态和粒径;利用酶联免疫吸附实验动态检测成骨生长肽壳聚糖-海藻酸钠微球的载药率、包封率和缓释规律。结果与结论:乳化交联法制备的壳聚糖-海藻酸钠微球,球形良好,球体表面有较多微孔,具有较高的包封率(>72%)。体外药物释放实验表明,成骨生长肽可以从壳聚糖-海藻酸钠微球中缓慢释放,整个释放过程可达49d,累积释放率>85%。提示应用乳化交联法制备的负载成骨生长肽壳聚糖-海藻酸钠缓释微球,具有很好的控制释放成骨生长肽的能力。

Preparation and in vitro detection of osteogenic growth peptide chitosan-alginate microspheres

BACKGROUND:In vitro injection of osteogenic growth peptide(OGP) can regulate the peripheral blood and proliferation of bone marrow cells to increase bone formation and accelerate fracture healing,but it can not be worldly used for its instability and inconvenience of injection.OBJECTIVE:To prepare the OGP chitosan-alginate microsphere by emulsion crosslinking,and to detect its particle size,drug loading,in vitro release,physical and chemical properties.METHODS:The OGP loaded chitosan-alginic acid microsphere was prepared using an emulsion cross-linking method with glutaral as the cross-linking agent.Microscopy and scanning electron microscopy were used to evaluate the morphological properties and particle size distribution.The drug loading,entrapment efficiency and in vitro drug release kinetics were detected by enzyme-linked immunosorbent assay.RESULTS AND CONCLUSION:The OGP loaded chitosan-alginic acid microspheres were spherical in shape,and showed a asperity surface with many micropores and a higher encapsulation efficiency(> 72%).From the in vitro release experiment,the OGP was controlled to release from the chitosan microsphere over 49 days and the release property of microspheres in vitro was well and the overall release rate was > 85%.It is indicated that the OGP loaded chitosan-alginic acid microsphere that is prepared by emulsion cross-linking method shows a good controlled release property.