Preparation of chitosan microparticles with acid-induced burst release property via electrospraying

doi:10.16085/j.issn.1000-6613.2015.10.030

Abstract

Abstract: Drug-loaded chitosan microparticles with acid-induced burst release property are successfully prepared by electrospraying technology. Chitosan aqueous solution containing cimetidine is used as the spray liquid and a mixture of toluene and n-hexanol is used as the collection solution. The effects of cross-linking degree on the drug entrapment efficiency and drug loading are systematically investigated. The results show that, when the cross-linker concentration is up to 2%, the highest drug entrapment efficiency and drug loading are obtained. Due to the use of terephthalaldehyde as cross-linker via forming Schiff base bonds, the prepared chitosan microparticles display rapid acid-triggered decomposition. As a result, the drug-loaded chitosan microparticles show acid-induced burst drug release in simulated gastric acid solution with pH of 2 and 37℃ within 1min. The prepared chitosan microparticles with acid-induced burst release property are promising as gastric drug delivery systems.

Key words: particle formation, pharmaceuticals, support, chitosan microparticles, acid-induced burst release, electrospraying

摘要： 利用静电喷射技术,以西咪替丁作为模型药物,混有药物的壳聚糖水溶液作为喷射液,甲苯/正己醇的混合溶液作为接收液,成功制备得到可在酸性条件下溶解并突释给药的壳聚糖载药微颗粒。系统考察了交联剂含量对壳聚糖微颗粒的药物包封率以及载药量的影响,并研究了壳聚糖微颗粒在酸性条件下的溶解特性以及在体外的突释给药效果。结果表明,当交联剂质量分数为2%时,壳聚糖微颗粒的包封率及载药量最大,分别为80%和3.8%。由于对苯二甲醛与壳聚糖交联形成的Schiff-base结构,使得壳聚糖微颗粒能够在中性条件下保持结构完整,而在酸性条件下由于Schiff-base结构的不稳定性致使微颗粒迅速溶解。因此,体外释药实验结果显示,在pH = 2、37℃的模拟胃酸溶液中,1min内壳聚糖微颗粒即可达到最大释药效果,而在pH = 6.4、37℃的水溶液中,壳聚糖微颗粒可以较长时间保持稳定,药物释放缓慢。这种具有酸致突释释药性能的壳聚糖微粒载体在胃部给药系统方面有良好的应用前景。

关键词: 粒子形成, 药物, 载体, 壳聚糖微颗粒, 酸致突释, 静电喷射

CLC Number:

TQ469

WANG Xiaoxue, JU Xiaojie, CHU Liangyin, XIE Rui, WANG Wei, LIU Zhuang. Preparation of chitosan microparticles with acid-induced burst release property via electrospraying[J]. Chemical Industry and Engineering Progree, 2015, 34(10): 3712-3718.

王小雪, 巨晓洁, 褚良银, 谢锐, 汪伟, 刘壮. 静电喷射技术制备可酸致突释给药的壳聚糖微颗粒[J]. 化工进展, 2015, 34(10): 3712-3718.

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