壳聚糖修饰的丹皮酚PEG-PLGA纳米粒的制备及其体外释药性能考察

目的:制备壳聚糖修饰的丹皮酚聚乙二醇-(聚乳酸-羟基乙酸共聚物)(PEG-PLGA)纳米粒,对其体外性质进行表征,考察纳米粒的体外释药性能,为丹皮酚的新型纳米制剂研究提供参考。方法:以PEG-PLGA为载体材料,壳聚糖为表面修饰剂,采用纳米沉淀法制备了壳聚糖修饰的丹皮酚PEG-PLGA纳米粒,利用正交试验优化处方工艺,并对其体外性质进行表征。以p H 7.4磷酸盐缓冲液为释放介质,考察壳聚糖修饰的丹皮酚PEG-PLGA纳米粒的体外释药行为。结果:载药纳米粒经壳聚糖修饰后,Zeta电位由负电荷转为正电荷且更加稳定,粒径略有增加。制备出的纳米粒外观呈球形,平均粒径和Zeta电位分别为(96.6±3.2)nm,(30.61±0.34)m V,载药量及包封率分别为10.87%和79.37%。体外释药试验表明载药纳米粒24 h的累计释放率62.4%。结论:按优选的处方成功制备了壳聚糖修饰的丹皮酚PEG-PLGA纳米粒,该制剂的体外性质良好且具有一定的缓释特性。

Preparation and in Vitro Release Properties of Paeonol-loaded PEG-PLGA Nanoparticles Modified by Chitosan

Objective: To prepare paeonol-loaded polyethylene glycol (PEG)-poly(lactic-co-glycolic acid) (PLGA) nanoparticles modified by chitosan and investigate its in vitro release behavior. Method: Taking PEG-PLGA as carrier material,chitosan as surface modifier,paeonol-loaded PEG-PLGA nanoparticles modified by chitosan was prepared by nano precipitation method,formulation of this preparation was optimized by orthogonal design,characteristics of nanoparticles were evaluated.In vitro release of this preparation was characterized with phosphate buffer (pH 7.4) as medium. Result: After being modified by chitosan,particle size of paeonol-loaded PEG-PLGA nanoparticles increased,while its Zeta potential turned to positive charge,its shape was spherical.Mean particle size,Zeta potential,drug loading efficiency and encapsulation efficiency were (96.6±3.2) nm,(30.61±0.34) mV,10.87% and 79.37%.Accumulated release rate of this nanoparticles reached 62.4% at 24 h. Conclusion: Paeonol-loaded PEG-PLGA nanoparticles modified by chitosan is prepared successfully,which shows a sustained-release characteristics with good in vitro properties.