化工学报 ›› 2020, Vol. 71 ›› Issue (8): 3797-3806.DOI: 10.11949/0438-1157.20200418

• 材料化学工程与纳米技术 • 上一篇    下一篇

肠靶向海藻酸钙基微胶囊的制备及控释性能研究

温霜1(),巨晓洁1,2(),谢锐1,2,汪伟1,2,刘壮1,2,褚良银1,2   

  1. 1.四川大学化学工程学院,四川 成都 610065
    2.四川大学高分子材料工程国家重点实验室,四川 成都 610065
  • 收稿日期:2020-04-21 修回日期:2020-05-13 出版日期:2020-08-05 发布日期:2020-08-05
  • 通讯作者: 巨晓洁
  • 作者简介:温霜(1995—),女,硕士研究生,577898496@qq.com
  • 基金资助:
    四川省青年科技基金杰出青年科技人才项目(2017JQ0027);霍英东教育基金会高等院校青年教师基金项目(151070)

Fabrication and controlled-release properties of intestinal-targeted Ca-alginate-based capsules

Shuang WEN1(),Xiaojie JU1,2(),Rui XIE1,2,Wei WANG1,2,Zhuang LIU1,2,Liangyin CHU1,2   

  1. 1.School of Chemical Engineering, Sichuan University, Chengdu 610065, Sichuan, China
    2.State Key Laboratory of Polymer Materials Engineering, Sichuan University, Chengdu 610065, Sichuan, China
  • Received:2020-04-21 Revised:2020-05-13 Online:2020-08-05 Published:2020-08-05
  • Contact: Xiaojie JU

摘要:

利用毛细管共挤出技术结合静电吸附和仿生硅化的方法,制备了海藻酸钙-壳聚糖/精蛋白/二氧化硅(ACPSi)复合微胶囊。ACPSi复合微胶囊的平均粒径约3.18 mm,单分散性好,囊壁最外层的二氧化硅层可抑制其在肠液pH环境中的溶胀,增强囊的机械稳定性。将羟丙甲基纤维素邻苯二甲酸酯(HPMCP)肠溶微球作为释药“微阀门”,嵌入囊壁可以更好地控制微胶囊的释药行为。以吲哚美辛为模型药物,当药物浓度为22.5 mg/ml时,ACPSi载药微胶囊在pH 2.5模拟胃液中3 h时累计释药率仅为0.33%,而转移至pH 6.8模拟肠液中19 h时累计释药率为77.78%;囊壁嵌入HPMCP微球后,22 h时累计释药率可提高约4%。因此,该复合微胶囊具有良好的肠靶向作用和控释特性,作为口服肠靶向缓控释制剂具有良好的应用前景。

关键词: 微胶囊, 肠靶向, 控制释放, 海藻酸钙, 微流体学, 药物, 传质

Abstract:

Ca-alginate-chitosan/protamine/silica (ACPSi) composite microcapsules were prepared by using capillary coextrusion technology combined with electrostatic adsorption and bionic silicification. The prepared composite ACPSi capsules have good monodispersity and the average particle size is about 3.18 mm. The rigid outer silica layer of the microcapsules can effectively inhibit the capsule swelling at pH 6.8 to improve the mechanical stability of the microcapsules. In addition, drug release behavior of microcapsules can be further controlled by embedding HPMCP enteric microspheres into the shell of ACPSi capsules as “micro-valves”. When the concentration of indomethacin is 22.5 mg/ml, the cumulative release rate of the ACPSi capsules is 0.33% at pH 2.5 for 3 h, after transferring to pH 6.8 buffer solution for 19 h, the cumulative release rate reaches 77.78%. The cumulative release rate can be increased by about 4% when HPMCP microspheres embedded into the capsule shell. The proposed ACPSi composite capsules exhibit good intestinal-targeted controlled-release performance, which provides a new strategy for developing oral intestinal-targeted drug delivery systems.

Key words: capsules, intestinal-targeted delivery, controlled-release, Ca-alginate, microfluidics, pharmaceuticals, mass transfer

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