载牛血清白蛋白壳聚糖微球的制备及其体外释药特性评价

Preparation of bovine serum albumin chitosan microspheres and evaluation of its drug release characteristics in vitro

目的:优化载牛血清白蛋白壳聚糖微球的制备工艺,并考察其体外释药特性,从而提高蛋白药物的稳定性,控制其释放速度,延长药物作用时间,提高药物生物利用度。方法:以高分子天然材料壳聚糖为载体,以离子凝胶法制备载牛血清白蛋白壳聚糖微球,通过单因素实验和正交实验设计优化制备工艺,并考察其体外释放特性。结果:扫描电子显微镜观察载牛血清白蛋白壳聚糖微球具有明显的球状结构;其最佳制备工艺为:壳聚糖分子量为300 ku、三聚磷酸钠浓度为10 mg/m L、壳聚糖浓度为3 mg/m L、牛血清白蛋白用量为30 mg,制备的微球载药率可达30.13%,体外释放可持续48 h,累积释放率达到70%,具有良好的缓释效果。结论:载牛血清白蛋白壳聚糖微球具有较高的载药量,缓释效果明显,为壳聚糖作为药物缓控释载体的进一步研究提供依据。

objective：To optimize the preparation technology of bovine serum albumin chitosan microspheres and investigate the drug release characteristics in vitro, in order to improve the stability of protein drugs, control the drug release rate, prolong the time of drug action and improve the bioavailability of drugs. Methods： Natural polymer chitesan were used as the material,the bovine serum albumin chitosan microspheres were prepared by ionic gelation method, the single factor test and orthogonal design were used to optimize the technology of preparation,and the characteristics of the study were also investigated in vitro release. Results Laser scanning microscope was for encapsulation of the bovine serum albumin chitosan microspheres. The best preparation technology were chitosan molecular of 300 ku, the concentration of sodium tripolyphosphate of 10 mg/mL, the concentration of chitosan of 3 mg/mL, the amount of bovine serum albumin of 30 mg. Under this condition, the microsphere drug loading rate was 30.13% ,and the in vitro release studies showed that 70% of BSA was released from the bovine serum albumin chitosan microspheres in the first 48 h which confirmed a good sustained-release effect and sustained release characteristics.Conclusion： The bovine serum albumin chitosan microspheres with high drug-loading content and obvious slow release effect can provide the basis for further research.