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载有川芎嗪的热敏性泊洛沙姆水凝胶的控释及抗炎活性

The Controlled Release and Anti-Inflammatory Activity of a Tetramethylpyrazine-Loaded Thermosensitive Poloxamer Hydrogel.

作者信息

Xia Hongmei, Jin Hongliu, Cheng Yongfeng, Cheng Zhiqing, Xu Yinxiang

机构信息

College of Pharmacy, Anhui University of Chinese Medicine, Hefei, 230038, People's Republic of China.

School of Life Science, University of Science and Technology of China, Hefei, 230027, People's Republic of China.

出版信息

Pharm Res. 2019 Feb 19;36(4):52. doi: 10.1007/s11095-019-2580-0.

Abstract

PURPOSE

Tetramethylpyrazine-loaded poloxamer hydrogel materials were studied to achieve the controlled release of tetramethylpyrazine.

METHODS

First, hydrogels having different concentrations of poloxamer 407 and poloxamer 188 were prepared. The gelling temperature and viscosity were measured. Second, we investigated the tetramethylpyrazine release rate from the thermosensitive poloxamer hydrogel materials in vitro and ex vivo. Finally, further study of the pharmacological efficacy of the tetramethylpyrazine-loaded thermosensitive poloxamer hydrogel materials was also investigated in vivo.

RESULTS

The in vitro, ex vivo and in vivo experimental results showed that the tetramethylpyrazine-loaded poloxamer hydrogel with the appropriate gelling temperature, good adhesion and easy preparation controlled the release of tetramethylpyrazine.

CONCLUSIONS

The hydrogel with the suitable nasal temperature and a satisfactory adhesion was selected. The relevant tests were carried out, including the determination of the concentration of drugs in the brain homogenate and the anti-inflammatory test after different modes of administration. So the poloxamer hydrogel was a novel carrier to deliver TMP to pass across the blood brain barrier via nasal administration.

摘要

目的

研究载有川芎嗪的泊洛沙姆水凝胶材料以实现川芎嗪的控释。

方法

首先,制备具有不同浓度泊洛沙姆407和泊洛沙姆188的水凝胶。测量其胶凝温度和粘度。其次,我们在体外和离体条件下研究了热敏性泊洛沙姆水凝胶材料中川芎嗪的释放速率。最后,还在体内研究了载有川芎嗪的热敏性泊洛沙姆水凝胶材料的药理功效。

结果

体外、离体和体内实验结果表明,具有合适胶凝温度、良好粘附性且易于制备的载有川芎嗪的泊洛沙姆水凝胶可控制川芎嗪的释放。

结论

选择了具有适宜鼻腔温度和良好粘附性的水凝胶。进行了相关试验,包括脑匀浆中药物浓度的测定以及不同给药方式后的抗炎试验。因此,泊洛沙姆水凝胶是一种新型载体,可通过鼻腔给药使川芎嗪穿过血脑屏障。

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