李伟泽, 赵宁, 陈卓, 韩文霞, 付丽娜, 何树苗, 傅文博, 贺升升, 李健. 基于白及多糖的苦参碱微球的制备J. 药学学报, 2018,53(2): 284-290. doi: 10.16438/j.0513-4870.2017-0903
引用本文: 李伟泽, 赵宁, 陈卓, 韩文霞, 付丽娜, 何树苗, 傅文博, 贺升升, 李健. 基于白及多糖的苦参碱微球的制备J. 药学学报, 2018,53(2): 284-290. doi: 10.16438/j.0513-4870.2017-0903
LI Wei-ze, ZHAO Ning, CHEN Zhuo, HAN Wen-xia, FU Li-na, HE Shu-miao, FU Wen-bo, HE Sheng-sheng, LI Jian. Preparation of matrine loaded microspheres based on Bletilla striata polysaccharideJ. Acta Pharmaceutica Sinica, 2018,53(2): 284-290. doi: 10.16438/j.0513-4870.2017-0903
Citation: LI Wei-ze, ZHAO Ning, CHEN Zhuo, HAN Wen-xia, FU Li-na, HE Shu-miao, FU Wen-bo, HE Sheng-sheng, LI Jian. Preparation of matrine loaded microspheres based on Bletilla striata polysaccharideJ. Acta Pharmaceutica Sinica, 2018,53(2): 284-290. doi: 10.16438/j.0513-4870.2017-0903

基于白及多糖的苦参碱微球的制备

Preparation of matrine loaded microspheres based on Bletilla striata polysaccharide

  • 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。

     

    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. These results indicate that the ME-BSPMS may be a promising transarterial chemoembolization carrier for cancer treatment.

     

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