Modern Medical Research Center, Third Affiliated Hospital of Soochow University, #185 Yuqian Road, Changzhou, China.
J Pharm Pharmacol. 2013 Jun;65(6):807-16. doi: 10.1111/jphp.12043. Epub 2013 Feb 26.
The aim of this study was to develop a curcumin intranasal thermosensitive hydrogel and to improve its brain targeting efficiency.
The hydrogel gelation temperature, gelation time, drug release and mucociliary toxicity characteristics as well as the nose-to-brain transport in the rat model were evaluated.
The developed nasal hydrogel, composed of Pluronic F127 and Poloxamer 188, had shorter gelation time, longer mucociliary transport time and produced prolonged curcumin retention in the rat nasal cavity at body temperature. The hydrogel release mechanism was diffusion-controlled drug release, evaluated by the dialysis membrane method, but dissolution-controlled release when evaluated by the membraneless method. A mucociliary toxicity study revealed that the hydrogel maintained nasal mucosal integrity until 14 days after application. The drug-targeting efficiencies for the drug in the cerebrum, cerebellum, hippocampus and olfactory bulb after intranasal administration of the curcumin hydrogel were 1.82, 2.05, 2.07 and 1.51 times that after intravenous administration of the curcumin solution injection, respectively, indicating that the hydrogel significantly increased the distribution of curcumin into the rat brain tissue, especially into the cerebellum and hippocampus.
A thermosensitive curcumin nasal gel was developed with favourable gelation, release properties, biological safety and enhanced brain-uptake efficiency.
本研究旨在开发一种姜黄素鼻用温敏水凝胶，并提高其脑靶向效率。
评价了水凝胶的胶凝温度、胶凝时间、药物释放和黏液纤毛毒性特征，以及在大鼠模型中的鼻内递药。
所开发的鼻用温敏水凝胶由 Pluronic F127 和 Poloxamer 188 组成，具有较短的胶凝时间、较长的黏液纤毛转运时间，并使姜黄素在体温下在大鼠鼻腔中的保留时间延长。水凝胶的释放机制通过透析膜法评估为扩散控制药物释放，但通过无膜法评估为溶解控制释放。黏液纤毛毒性研究表明，水凝胶在应用后 14 天内仍能保持鼻黏膜完整性。与姜黄素溶液注射的静脉给药相比，姜黄素水凝胶经鼻给药后脑组织中姜黄素的药物靶向效率在大脑、小脑、海马和嗅球中分别为 1.82、2.05、2.07 和 1.51 倍，表明水凝胶显著增加了姜黄素向大鼠脑组织的分布，特别是小脑和海马。
开发了一种具有良好胶凝、释放性能、生物安全性和增强脑摄取效率的姜黄素鼻用温敏凝胶。
