氢化泼尼松-羟基丁酸酯-羟基戊酸酯共聚物纳米粒制备与性质

目的用新型生物可降解材料羟基丁酸酯-羟基戊酸酯共聚物(PHBV)为载体,以氢化泼尼松(prednisolone,PNS)为模型药制备PNS-PHBV纳米粒(NP)。方法用超声乳化法制备PNS-PNBV纳米粒,激光粒度分析仪测试NP的粒径及其分布以及粒子表面的Zeta电位。结果NP的粒径为50～250 nm。随着药/载比增加,NP的载药量也增大,但包封率与Zeta电位却明显下降;体外释药曲线表现出明显两相释药特征,伴随着不同程度突释效应,粒径越小突释效应越大,体外释药最长达32 h。结论PNS-PNBV纳米粒制备工艺稳定,具有明显缓释作用。

PREPARATION AND CHARACTERIZATION OF PREDNISOLONE-POLY (HYDROXYBUTYRATE-CO-HYDROXYVALERATE) NANOPARTICLES

AIM: To optimize the preparation of sustained release prednisolone-poly (hydroxybutyrate-cohydroxyvalerate) (PNS-PHBV) nanospheres (NP) using the novel biodegradable materials PHBV as the carriers and PNS as a model drug. METHODS: PNS-PHBV nanospheres were prepared by ultrasonic-emulsion technique. The diameter, its distribution and Zeta potential on the surface of particles were measured by means of Zetasizer. RESULTS: The diameter of NP is in the range of 50-250 nm. The drug loading of NP increases but incorporation efficiency and Zeta potential dramatically decrease with increasing ratio of the feeding quantities of drug to those of carriers. The drug release behavior in vitro appeared to have biphasic characteristics with initial burst effect. The more burst effect, the less the diameters of nanoparticles. The longest release time was up to 32 h. CONCLUSION: The technology of preparation is reasonable and PNS-PHBV nanoparticle showed significant sustained release.