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作 者:李海霞[1] 杨耀[1] 路春波 罗政[1] 张振中[1]
机构地区:[1]郑州大学药学院,郑州450001
出 处:《郑州大学学报(医学版)》2015年第5期682-686,共5页Journal of Zhengzhou University(Medical Sciences)
基 金:郑州市科技局科技攻关项目0910SGYS33389-9
摘 要:目的:采用主动载药法制备芦丁纳米脂质体,提高包封率,增加药物在体外的释放。方法:利用醋酸钙梯度造成主动载药的驱动力,HPLC测定芦丁含量,离心超滤法测定脂质体包封率,激光粒度仪测定粒径分布和电位,考察单因素对包封率及粒径的影响,并进一步研究芦丁纳米脂质体在4℃的稳定性和体外释放。结果:空白脂质体10倍体积的30 g/L蔗糖、透析3次可高效建立醋酸钙梯度,20 g/L PVP作为溶解介质可有效增加芦丁的包封率和稳定性,在最佳制备工艺条件(磷脂浓度40 g/L、磷脂∶胆固醇质量比为5∶1、药脂质量比1∶30、50℃孵育15 min,包封率达80.3%)下成品脂质体平均粒径为185 nm,电位-1.2 m V,28 d稳定性良好,体外释放较完全。结论:醋酸钙梯度主动载药法可制备高包封率、释药较完全的芦丁纳米脂质体。Aim:To prepare nanoliposomes with high entrapment efficiencies ( EE) by active loading drug method for improving absorption of rutin in the body .Methods:The gradient of calcium acetate was used to produce the driving force of loading drug .HPLC, centrifugal ultrafiltration and laser particle size analyzer were employed to determined rutin con -tent, EE, size distribution and zeta potential , respectively .The influence of various factors on the EE and size was investi-gated.Furthermore, the release behavior in vitro and stability under 4℃were studied.Results:The conditions of genera-ting calcium acetate gradient were determined as 10 volumes of 30 g/L sucrose to dialyze three times .The EE and stability of liposomes were enhanced by 20 g/L PVP solubilizing rutin .Under the optimized preparation conditions ( phospholipid con-centration 40 g/L, phospholipid:cholesterol 5:1, drug-lipid ratio 1:30, 50 ℃ incubation foe 15 min), the EE a-chieved 80.3%.Rutin was nanosized with an average size of 185 nm, a zeta potential of -1.2 mV.Also, the preparation was stable within 28 days and more drug was released compared with native rutin .Conclusion:Active loading druy method of calcium acetate gradient can prepare rutin nanoliposomes with high EE and better release .
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