温敏型姜黄素鼻用原位凝胶增强脑靶向性  

Enhanced Brain Targeting of Curcumin by Intranasal Administration of a Thermosensitive Poloxamer Hydrogel

作　　者：陈溪[1] 杨洪斌[2] 胡一桥[2] 杨伊林[3] 支枫[3] 汤卫国 周建平[1] 

机构地区：[1]中国药科大学药学院,南京210009 [2]南京大学生命科学院,南京210093 [3]常州市第一人民医院神经外科现代医学研究中心,常州213003 [4]金陵制药厂,南京210038

出　　处：《药学与临床研究》2013年第1期9-12,共4页Pharmaceutical and Clinical Research

基　　金：2010年常州市生物技术及制药科技专项(CE20105006)

摘　　要：目的:制备温度敏感型的姜黄素鼻用凝胶制剂,以提高姜黄素的脑部生物利用度。方法:通过粘度实验进行原位凝胶制剂的处方筛选,以胶凝时间、胶凝温度等为指标,优化处方;采用透析袋法考察原位凝胶的体外释放;以大鼠为模型,考察姜黄素原位凝胶的脑靶向性及脑内分布,并与其静脉注射剂相比较。结果:姜黄素原位凝胶剂优化处方具有最短的胶凝时间,可以长时间粘附在鼻腔粘膜上;释放行为属于Fickian扩散机制;姜黄素脑内分布试验表明,原位凝胶在大脑、小脑、海马、嗅球中的药物靶向效率(DTE)分别为静脉给药的1.82、2.05、2.07、1.51倍,说明原位凝胶给药显著增强了姜黄素的脑靶向性。结论:制备的姜黄素原位凝胶剂具有温度敏感的特点,并显著提高了姜黄素的脑靶向性。Objective： The aim of this study is to develop a curcumin intranasal thermosensitivc hydrogel and to improve its brain targeting efficiency. Methods： The hydroge｜ gelation temperature and time, the drug release characteristics as well as nose-to-brain transport in a rat model were evaluated. Results： The developed nasal hydrogel composed of Pluronic F127 （PF-127） and Poloxamer 188 （P188） had a shorter gelation time and a longer mucociliary transport time compared with curcumin solution. The hydrogel showed diffusion-controlled drug release drug targeting efficiency （DTE） for the drug in when evaluated using the dialysis membrane method. The the cerebrum, cerebellum, hippocampus and olfactory bulb after intranasal administration of the curcumin hydrogel were respectively 1.82, 2.05, 2.07 and 1.51 times over those after intravenous administration of the curcumin solution injection, indicating that the hydrogel significantly increased the distribution of thermosensitive curcumin nasal gel has been enhanced brain uptake efficiency. curcumin into the rat brain tissues. Conclusion： developed with favorable gelation, release properties The and

关 键 词：姜黄素 原位凝胶 脑靶向 

分 类 号：R944.15[医药卫生—药剂学]