[1]李海霞,杨 耀,路春波,等.醋酸钙梯度主动载药法制备芦丁纳米脂质体[J].郑州大学学报(医学版),2015,(05):682-685.
 LI Haixia,YANG Yao,LU Chunbo,et al.Loading rutin into nanoliposomes by forming calcium acetate gradient and its quality evaluation[J].JOURNAL OF ZHENGZHOU UNIVERSITY(MEDICAL SCIENCES),2015,(05):682-685.
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醋酸钙梯度主动载药法制备芦丁纳米脂质体()
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《郑州大学学报(医学版)》[ISSN:1671-6825/CN:41-1340/R]

卷:
期数:
2015年05期
页码:
682-685
栏目:
应用研究
出版日期:
2015-09-20

文章信息/Info

Title:
Loading rutin into nanoliposomes by forming calcium acetate gradient and its quality evaluation
作者:
李海霞杨 耀路春波罗 政张振中#
郑州大学药学院 郑州 450001
Author(s):
LI HaixiaYANG YaoLU ChunboLUO ZhengZHANG Zhenzhong
School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001
关键词:
芦丁 醋酸钙梯度 纳米脂质体 主动载药法 包封率
Keywords:
rutin calcium acetate gradient nanoliposome active loading drug method entrapment efficiency
分类号:
R944.9
文献标志码:
A
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GA6FA胆固醇质量比为5GA6FA1、药脂质量比1GA6FA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 mV,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。
Abstract:
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 content, EE, size distribution and zeta potential, respectively. The influence of various factors on the EE and size was investigated. Furthermore, the release behavior in vitro and stability under 4 ℃ were studied.Results: The conditions of generating 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 concentration 40 g/L, phospholipidGA6FAcholesterol 5GA6FA1, drug-lipid ratio 1GA6FA30, 50 ℃ incubation foe 15 min), the EE a------------------------------------------------ *郑州市科技局科技攻关项目 0910SGYS33389-9 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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更新日期/Last Update: 1900-01-01