Preparation of calcium alginate/halloysite drug-loaded microspheres and its sustained-release properties for metformin hydrochloride

doi:10.16085/j.issn.1000-6613.2017-2127

Abstract

Abstract: Sustained-release can improve the drug utilization rate and reduce its toxicity. Calcium alginate/halloysite drug loaded microspheres were prepared by cross-linking method. The preparation conditions and release properties of drug loaded microspheres were investigated by the entrapment efficiency and the release effect of metformin hydrochloride (MH). The as-prepared microspheres were characterized by SEM, FTIR and TGA. The results showed that the microspheres had a better encapsulation efficiency (79.23%) under optimum prepare conditions that the cross linking temperature was 0℃, the amount of sodium alginate was 1g and the amount of halloysite was 2g, respectively. The prepared drug-loaded microspheres showed good pH sensitivity and sustained release effect, and they could be effectively released in phosphate buffer of pH=6.8, and the sustained release rate reached 85.83% within 720min. The calcium alginate solidified particles and halloysite formed composite structure in drug-loaded microsphere demonstrated by SEM images. The FTIR results showed that MH was mainly distributed in drug loaded microspheres in the form of physical embedding. The TGA results demonstrated that adding halloysite can improve the thermal stability of composites over 200℃.

Key words: halloysite, calcium alginate, metformin hydrochloride, sustained-release

摘要： 缓释可提高药物利用率，降低其毒副作用。采用交联法制备了海藻酸钙/埃洛石载药微球，以载药微球对盐酸二甲双胍（MH）药物的包封率和缓释效果为考察对象，研究了载药微球的制备工艺和缓释性能，并通过SEM、FTIR和TGA对其结构进行了表征。结果表明：在交联温度为0℃、海藻酸钠用量为1g、埃洛石添加量为2g时，能得到较优的载药微球包封率（79.23%）。上述条件下制得的复合载药微球在pH=6.8的磷酸盐缓冲液中能有效缓释，且720min后缓释度可达85.83%，说明其具有较好的pH敏感性和缓释效果。SEM表明海藻酸钙颗粒与埃洛石在载药微球内部形成复合结构，FTIR表明MH主要以物理包埋的形式于载药微球中，TGA表明添加埃洛石可以提高复合材料在200℃以上的热稳定性。

关键词: 埃洛石, 海藻酸钙, 盐酸二甲双胍, 缓释

CLC Number:

TD985

SUN Qing, LUO Wei, ZHANG Jian, SHENG Jiawei. Preparation of calcium alginate/halloysite drug-loaded microspheres and its sustained-release properties for metformin hydrochloride[J]. Chemical Industry and Engineering Progress, 2018, 37(08): 3138-3145.

孙青, 罗威, 张俭, 盛嘉伟. 海藻酸钙/埃洛石载药微球的制备与缓释盐酸二甲双胍性能[J]. 化工进展, 2018, 37(08): 3138-3145.

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