Thermosensitive chitosan-based hydrogel containing liposomes for the delivery of hydrophilic molecules
Thermosensitive chitosan-based hydrogel containing liposomes for the delivery of hydrophilic molecules
复制标题
DOI：
10.1016/s0168-3659(02)00146-3
复制
发表时间：
2002-08-21
影响因子：
10.8
通讯作者：
Leroux, JC
中科院分区：
文献类型：
--
作者：
Ruel-Gariépy, E;Leclair, G;Leroux, JC
最近提出了一种新的可注射的原位凝胶化温敏性壳聚糖-β-甘油磷酸盐（C-GP）制剂用于组织修复和药物递送。该系统可以在几小时到几天的时间内持续释放大分子。然而，对于低分子量亲水性化合物，释放通常在24小时内完成。在这项研究中，脂质体被添加到C-GP的解决方案和他们的粘弹性的系统和释放动力学的封装羧基荧光素的影响进行了研究。脂质体的存在使凝胶化速率和凝胶强度略有增加。体外释放曲线表明在至少2周内受控递送。释放速率强烈依赖于脂质体的大小和组成（即添加胆固醇），并在释放介质中磷脂酶的存在。当使用用带负电荷的脂质或具有高相变温度的脂质制备的脂质体时，动力学基本上没有改变。这些结果表明，脂质体-C-GP系统在体温下快速凝胶化，并且可以持续递送低分子量亲水性化合物。提出了一个数学模型来表征释放动力学。(C)2002 Elsevier Science B. V.保留所有权利。
A novel injectable in situ gelling thermosensitive chitosan-beta-glycerophosphate (C-GP) formulation has been recently proposed for tissue repair and drug delivery. The system can sustain the release of macromolecules over a period of several hours to a few days. However, with low-molecular-weight hydrophilic compounds, the release, is generally completed within 24 h. In this study, liposomes were added to the C-GP solution and their effect on the viscoelastic properties of the system and release kinetics of encapsulated carboxyfluorescein was investigated. The gelation rate and gel strength were slightly increased by the presence of the liposomes. The in vitro release profiles demonstrated controlled delivery over at least 2 weeks. The release rate strongly depended on the liposome size and composition (i.e. addition of cholesterol), and on the presence of phospholipase in the release medium. The kinetics was not substantially modified when using liposomes prepared with a negatively-charged lipid or a lipid having a high phase transition temperature. These results indicate that the liposome-C-GP system rapidly gels at body temperature, and can sustain the delivery of low-molecular-weight hydrophilic compounds. A mathematical model was proposed to characterize the release kinetics. (C) 2002 Elsevier Science B.V. All rights reserved.