文章摘要
竹节参皂苷Ⅳa纳米体系对脑梗死的靶向治疗*
Nanoparticles of Chikusetsu Saponin Ⅳa for targeting therapy of cerebral infarction
投稿时间:2019-11-25  修订日期:2019-12-10
DOI:
中文关键词: 脑梗死  纳米疗法  脂质-聚合物杂化纳米粒  乳铁蛋白  竹节参皂苷Ⅳa
英文关键词: Cerebral infarction  Nano-therapy  Hybrid lipid-polymer nanoparticles  Lactoferrin  Chikusetsu saponin Ⅳa
基金项目:国家自然科学基金(NO.81603325)
作者单位E-mail
吴忻晶 1.空军军医大学第一附属医院药剂科2.山西省运城市中心医院药学部 345389469@qq.com 
关月△ 空军军医大学第一附属医院药剂科 23395691@qq.com 
郭桂萍 空军军医大学第一附属医院药剂科  
曹珊珊 空军军医大学第一附属医院药剂科  
葛洁 空军军医大学第一附属医院药剂科  
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中文摘要:
      目的:制备和评价以乳铁蛋白修饰的,荷载竹节参皂苷Ⅳa的脂质-聚合物杂化纳米体系(Lactoferrin-modified lipid-polymer hybrid nanoparticles as a carrier for brain delivery of Chikusetsu saponin Ⅳa,CⅣa/Lf-LPNs),用于脑梗死的靶向治疗。 方法:采用纳米沉淀法制备了CⅣa/Lf-LPNs、lipid-polymer hybrid nanoparticles loaded with Chikusetsu saponin IVa(CⅣa/LPNs)、lipid-polymer hybrid nanoparticles modified by coating with lactoferrin(Lf-LPNs),比较了它们的理化性质、体外释药性质、大鼠血液和脑中药物浓度变化及其对脑缺血模型大鼠的存活率和生化指标的影响。 结果:乳铁蛋白修饰为纳米制剂带来正电荷,并附着在纳米体系表面,增大了纳米粒子的直径。三种纳米制剂的包封率均为90%左右。CⅣa/Lf-LPNs具有更持久的药物释放行为。CⅣa/Lf-LPNs组和CⅣa/LPNs组的血药浓度曲线是相似的,但二者脑部药物浓度曲线不同,CⅣa/Lf-LPNs组几乎每个时间点的脑部药物浓度均高于CⅣa/LPNs组(P<0.05)。此外,CⅣa/Lf-LPNs组提高了脑缺血模型大鼠的存活率,LDH含量最低,对脑缺血脑梗死的改善效果显著高于CⅣa/LPNs和CⅣa溶液组(P<0.05)。 结论:本文制备的CⅣa/Lf-LPNs可有效传递药物到达脑部,并缓慢持续的发挥改善脑缺血脑梗死的作用,是一种极具潜力的脑靶向治疗体系。
英文摘要:
      Objective: Lactoferrin-modified lipid-polymer hybrid nanoparticles as a carrier for brain delivery of Chikusetsu saponin Ⅳa,CⅣa/Lf-LPNs)was prepared and evaluated for nano-targeted therapy for cerebral infarction. Methods: CⅣa/Lf-LPNs, lipid-polymer hybrid nanoparticles loaded with ginsenoside IVa(CⅣa/LPNs)and lipid-polymer hybrid nanoparticles modified by coating with lactoferrin(Lf-LPNs)were prepared by nano-precipitation method. The physical-chemical characteristics and drug release properties were examined in vitro. In vivo, the changes of drug concentrations in the blood and brain of cerebral ischemia model rats were compared. The survival rates and biochemical indexes in blood were also evaluated. Results: Lactoferrin modification was positively charged in the nanoformulation and attached to the surface of nanoparticle, increasing the diameter of the nanoparticles. The encapsulation efficiencies of three nano-formulations were all about 90%. CⅣa/Lf-LPNs performed a longer lasting drug release behavior. The drug concentration curves of CⅣa/Lf-LPNs group and CⅣa/LPNs group were similar in plasma, but different in brain. The brain drug concentrations in CⅣa/Lf-LPNs group were higher than those in CⅣa/LPNs group at almost every time point (P < 0.05). In addition, CⅣa/Lf-LPNs increased the survival rate and decreased LDH content of cerebral ischemia model rats. The improvement effect of CⅣa/ Lf-LPNs on cerebral ischemia and infarction was significantly higher than that of CⅣa/LPNs and CⅣa solution (P < 0.05). Conclusion: CⅣa/Lf-LPNs effectively delivered drugs to the brain, and played an efficient role inimproving cerebral ischemia and cerebral infarction. It might be a promising brain-targeted therapeutic system.
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