U0126纳米药物载体的制备及其用于肺动脉高压治疗  

U0126 delivery nanoparticles for treatment of pulmonary arterial hypertension

作　　者：李科[1] 徐仓宝[1] 张亚萍[1] 张彦[2] LI Ke;XU Cangbao;ZHANG Yaping;ZHANG Yan(Shaanxi Key Laboratory of Ischemic Cardiovascular Disease,Xi’an Medical University,Xi’an 710021,China;College of Pharmacy,Xi’an Medical University,Xi’an 710021,China)

机构地区：[1]西安医学院陕西省缺血性心血管疾病重点实验室,陕西西安710021 [2]西安医学院药学院,陕西西安710021

出　　处：《化工科技》2020年第4期28-35,共8页Science & Technology in Chemical Industry

基　　金：陕西省教育厅重点学科研究计划项目(18JS101);陕西省呼吸病预防与诊治工程研究中心开放基金项目(2017GCKF02)。

摘　　要：通过纳米载体增加抗收缩化合物U0126的生物利用度,以提高其抗肺动脉高压的效果。首先制备阳离子双亲淀粉包材,通过该材料构建U0126纳米药物载体,并检测其载药性能,利用体外肺动脉血管培养模型评价其在肺动脉高压治疗方面的效果。结果表明,所制备的阳离子双亲淀粉包材毒性低,可有效负载疏水性化合物U0126,载体为平均粒径(113±6.9)nm的球形胶束,包裹率达到(93.8±2.8)%,载药量为(17.4±4.6)%,在不同溶液环境中均具有良好的稳定性,且具有缓释效果。U0126纳米药物载体可有效积累于内皮细胞受损的血管壁内,而在正常血管壁中积累较少,较之游离U0126具有更好的干预效果。证明U0126纳米药物载体能显著提高药物对肺动脉高压的逆转效果。In order to enhance the treatment of pulmonary arterial hypertension(PAH),the nanocarrier was employed in delivery of U0126,which is an anti-constriction compound.Cationic amphiphilic starch was prepared and utilized for construction of U0126 delivery nanoparticles(U0126 NPs).The treatment effect of the U0126 NPs was evaluated by in vitro pulmonary arterial tissue culture model.The results indicated that cationic amphiphilic starch had low cytotoxicity,which could encapsulate U0126 effectively.The shape of U0126 NPs was spherical,and the size of the NPs was(113±6.9)nm.The maximal encapsulation efficiencies and drug loading of U0126 in the NPs were(93.8±2.8)%and(17.4±4.6)%,respectively.U0126 NPs showed great stability and sustained release.U0126 NPs could perform effective targeted delivery in the pulmonary arterial tissue culture model,and the NPs less accumulated in the normal arterial tissues.In comparison to treatment with the free drug,the U0126 NPs significantly enhanced the effect of anti-constriction in the arterial model.These results suggest that U0126 NPs have significant potential for the treatment of PAH.

关 键 词：肺动脉高压 纳米药物载体 U0126 抗收缩 

分 类 号：TQ460.1[化学工程—制药化工]