高等学校化学学报

高等学校化学学报 ›› 2013, Vol. 34 ›› Issue (5): 1174.doi: 10.7503/cjcu20120742

• 生物化学 • 上一篇    下一篇

基于纳米囊泡的原位凝胶系统

管清香1, 鲁晶雯1, 郭杰2, 宁兆伦3, 陈晨1, 尹建元1   

  1. 1. 吉林大学药学院, 长春 130021;
    2. 吉林大学第二临床医院, 长春 130023;
    3. 长春应用化学研究所, 长春 130024
  • 收稿日期:2012-08-09 出版日期:2013-05-10 发布日期:2013-05-10
  • 通讯作者: 郭 杰, 女, 博士, 副教授, 主要从事高分子材料在控释系统中的应用研究. E-mail: guojie@jlu.edu.cn E-mail:guojie@jlu.edu.cn
  • 基金资助:

    吉林省卫生厅项目(批准号: 2010Z104)和吉林大学交叉学科项目(批准号: 200903341)资助.

Investigation on in situ Gel Based on Liposomal Vesicle

GUAN Qing-Xiang1, LU Jing-Wen1, GUO Jie2, NING Zhao-Lun3, CHEN Chen1, YIN Jian-Yuan1   

  1. 1. School of Pharmacy, Jilin University, Changchun 130021, China;
    2. Department Radiotherapy, the Second Clinical Hospital, Jilin University, Changchun 130023, China;
    3. Changchun Institute of Applied Chemistry, Chinese Academy of Science, Changchun 130024, China
  • Received:2012-08-09 Online:2013-05-10 Published:2013-05-10
  • Contact: GUAN Qing-xiang E-mail:guojie@jlu.edu.cn

PDF (PC)

被引次数

4

摘要：

构建了纳米囊泡的原位凝胶系统. 以卵磷脂(PC)和胆固醇(CH)为纳米囊脂质材料, 按m(PC):m(CH)=3:1及m(脂质材料):m(药物)=5:1称取PC, CH和药物, 溶于无水乙醚作为有机相, 以质量分数为0.5%的吐温-80的磷酸盐(pH=7.4)缓冲液为水相(有机相与水相体积比为1.5:1), 采用薄膜分散-高压均质法制备了叶黄素纳米囊泡. 将普朗尼克F127(F127)和普朗尼克F68(F68)分散于纳米囊泡中水化, 制备了纳米囊泡原位凝胶系统. 以试管倒置法测定人工泪液和添加剂对F127-F68纳米囊泡原位凝胶系统胶凝温度的影响; 采用流变学研究了系统升温过程中溶胶-凝胶转变过程及上述辅料对该转变过程的影响; 分别以无膜溶蚀法和高效液相色谱(HPLC)法探讨了系统的体外溶蚀动力学和体外释药行为. 结果表明, 优化的纳米囊泡凝胶系统在25 ℃呈溶液态, 在眼部微环境下形成凝胶, 且药物释放及凝胶溶蚀均以恒定的速率进行, 为零级动力学特征.

关键词: 原位凝胶, 纳米囊泡, 眼部递放系统, 流变学

Abstract:

To develop a combination of lipid nanoparticle and polymer, liposomal vesicle was prepared by the film dispersion-high pressure homogeneous method, with lipid composition m(phosphatidyl choline):m(cholesterol)=3:1. Briefly, the organic phase containing m(lipid):m(lutein)=5:1 was dissolved in absolutely ether, the water phase was phosphate buffer containing 0.5% of Tween 80. The volume ratio of the former and the latter was 1.5:1. Liposomal vesicle in situ gel was developed by suspending F127 and F68 in liposomal vesicle. The effect of simulative tears and excipients on gelation temperature was determined by tube-reverse method and the sol-gel transition process during the heating was evaluated by rheological mea-sure. Erosion of the gel and drug release from the gel in vitro were measured by membrane-free and high performamce liquid chromatography(HPLC), respectively. The liposomal vesicle in gel in situ kept solution state at room temperature and immediately formed gel in eye microenvironment. Gel erosion and gel drug relaease in vitro were kept a constant rate and both of them showed zero-order kinetic characteristics. In conclusion, a novel drug delivery system, liposomal vesicle in gel in situ was developed and characterized.

Key words: In situ gel, Nanovesicle, Eye ophthalmic drug delivery system, Rheology

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