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聚电解质逐层组装的微凝胶脉冲制剂的体内外释放研究
周闺臣1,2,鲁莹1,张翮1,俞媛1,陈琰1,张国庆2,孙治国1,黄景彬1,于菲菲1,邹豪1*,钟延强1*
0
(1. 第二军医大学药学院药剂学教研室,上海 200433;
2. 第二军医大学东方肝胆外科医院药材科,上海 200438
*通信作者)
摘要:
目的 制备聚电解质逐层组装的壳聚糖海藻酸钠微凝胶,考察体外释放规律,观察体内释放过程。 方法 使用高压静电成囊机制备海藻酸钠壳聚糖微凝胶核心,通过静电吸附原理将聚电解质逐层包裹在微凝胶表面形成包衣层;考察不同物料比例、包衣层数对体外释药性能的影响;小鼠皮下注射制剂后,制备组织切片观察体内释放过程。 结果 海藻酸钠浓度、氯化钙浓度、聚电解质包衣层数影响脉冲释放时滞以及时滞后释放速度。 结论 聚电解质逐层组装的微凝胶脉冲制剂,体外释药性能可灵活调控,体内释药可见,并且制剂安全,生物相容性好。
关键词:  聚电解质  微凝胶  脉冲释药  FITC-dextran
DOI:10.3724/SP.J.1008.2011.01218
投稿时间:2011-07-21修订日期:2011-09-20
基金项目:国家自然科学基金(30801441).
Pulsed release behavior of microgels coated layer-by-layer by polyelectrolyte in vivo and in vitro
ZHOU Gui-chen1,2,LU Ying1,ZHANG He1,YU Yuan1,CHEN Yan1,ZHANG Guo-qing2,SUN Zhi-guo1,HUANG Jing-bin1,YU Fei-fei1,ZOU Hao1*,ZHONG Yan-qiang1*
(1. Department of Pharmaceutics, School of Pharmacy, Second Military Medical University, Shanghai 200433, China;
2. Department of Pharmacy, Eastern Hepatobiliary Surgery Hospital, Second Military Medical University, Shanghai 200438, China
*Corresponding author.)
Abstract:
Objective To investigate the in vitro and in vivo release of chitosan-alginate microgels coated layer-by-layer by polyelectrolyte self-assembly. Methods The cores of the microgels were made by gelatinization using electrostatic microencapsulated and coated by polyelectrolytes using electrostatic attraction.The effects of different layers and ratios of polymer on the in vitro release of FITC-dextran were evaluated. Histological examination was carried out to observe the in vivo release process by injecting the coated microgels into mice. Results The results showed that alginate and calcium chloride concentrations and polyelectrolyte layers markedly affected the lag time of pulsed release and the releasing speed after lagging. Conclusion The release of microgels coated layer-by-layer by polyelectrolyte can be controlled in vitro and can be observed in vivo; meanwhile, the microgels are safe and have good biocompatibility.
Key words:  polyelectrolyte  microgels  pulsed drug delivery  FITC-dextran