PDF《基于白及多糖的苦参碱微球的制备》

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284 ・ 药学学报 Acta Pharmaceutica Sinica 2018,

53 (2):

284 ?290 基于白及多糖的苦参碱微球的制备 李伟泽 1, 2* , 赵宁1,

2 , 陈卓1,

2 , 韩文霞

1 , 付丽娜 1,

2 , 何树苗

1 , 傅文博

1 , 贺升升

1 , 李健1(西安医学院 1.

药学院, 2. 药物研究所, 陕西 西安 710021) 摘要: 微球 (microspheres, MS) 是一种优良的经动脉化疗栓塞载体.本文以中药材白及 (Bletilla striata) 的 天然活性成分白及多糖 (Bletilla striata polysaccharide, BSP) 为骨架材料, 采用乳化?交联法制备了包载苦参碱 (matrine, ME) 的白及多糖微球 (matrine loaded Bletilla striata polysaccharide microspheres, ME-BSPMS), 并对 ME-BSPMS 的外观形态、粒度、载药量、吸水膨胀率、悬浮性、药物包埋情况与体外释药行为等药剂学性质进 行表征. 研究结果显示, ME-BSPMS 在扫描电镜 (SEM) 下呈表面光滑的规整球形结构, 平均粒径为 (85 ±7) μm;

其在生理盐水中悬浮性良好, 且20 min 内膨胀率达 (53 ±4.2) %;

ME-BSPMS 对ME 的载药量为 (30.12 ±3.25) %, 差示扫描量热仪 (DSC) 检测显示 ME 与BSP 相容性良好, ME 能充分被包埋于微球的骨架中;

12 h 时, ME-BSPMS 在生理盐水中的体外累积释药量为 (25.38 ± 1.57) %, 显示了良好的药物缓释行为.综上, 以BSP 为骨架材料的 微球制剂可为肿瘤的经动脉化疗栓塞疗法提供一种优良的新型血管栓塞载体. 关键词: 白及多糖;

苦参碱;

经动脉化疗栓塞;

微球;

制剂性能 中图分类号: R943 文献标识码: A 文章编号: 0513-4870 (2018) 02-0284-07 Preparation of matrine loaded microspheres based on Bletilla striata polysaccharide LI Wei-ze1, 2* , ZHAO Ning1,

2 , CHEN Zhuo1,

2 , HAN Wen-xia1 , FU Li-na1,

2 , HE Shu-miao1 , FU Wen-bo1 , HE Sheng-sheng1 , LI Jian1 (1. School of Pharmacy, 2. Institute of Medicine, Xi'

an Medical University, Xi'

an 710021, China) Abstract: Microspheres (MS) are an excellent transarterial chemoembolization carrier for cancer treatment. Then the Bletilla striata polysaccharide (BSP) that was isolated from the rattan of Bletilla striata was used as skeleton material, and the matrine (ME) loaded Bletilla striata polysaccharide microspheres (ME-BSPMS) were prepared by emulsify-chemical crosslinking method. ME-BSPMS was characterized for appearance shape, particle size, drug loading, swelling ratio, suspension property, drug entrapment condition and in vitro release characteristics. The results showed that the ME-BSPMS appeared as round spherical and smooth shape by SEM, with an average size of (85 ±7) μm. ME-BSPMS with a good suspension in physiological saline and the swelling ratio could reach upwards of (53 ±4.2) % in

20 minutes, also with a large amount of drug loading of (30.12 ±3.25) %. The results of DSC scanning indicate that good compatibility exists between the ME and BSP, and the ME could be embedded fully in the matrix of the ME-BSPMS. The accumulation drug release from ME-BSPMS was (25.38 ±1.57) % at

12 h, this suggests that the ME-BSPMS has a good sustained release effect. 收稿日期: 2017-09-12;

修回日期: 2017-10-09. 基金项目: 陕西省自然科学基金面上项目 (2017JM8109, 2017JM8023);

西安医学院省级重点学科?药学资助 (1007);

西安医学院药学省级重点学 科建设项目 (2016YXXK01, 2016YXXK07). *通讯作者 Tel: 86-29-86177546, E-mail: weizeli@126.com DOI: 10.16438/j.0513-4870.2017-0903 李伟泽等: 基于白及多糖的苦参碱微球的制备 ・