鼻用黄芩苷磷脂复合物原位凝胶脑靶向性研究

Evaluation of Brain-Targeting of Nasal Baicalin-Phospholipid Complex in Situ Gel

目的研究鼻用黄芩苷磷脂复合物原位凝胶在大鼠体内血液与脑组织中的药物分布,并评价其脑靶向性。方法大鼠静注黄芩苷磷脂复合物溶液,经鼻分别给予黄芩苷磷脂复合物混悬液和原位凝胶后,采用HPLC分别测定血浆中及脑组织中黄芩苷的浓度。结果与静注黄芩苷磷脂复合物溶液组相比,鼻用复合物混悬液和原位凝胶组大鼠脑组织中的药物分布显著增加,且原位凝胶组的脑靶向指数高于混悬液组,其嗅区转移率分别为88.8%,79.1%,药物平均滞留时间前者比后者增加近3倍。结论鼻用黄芩苷磷脂复合物混悬液和原位凝胶具有一定的脑靶向性,而原位凝胶的脑靶向作用强于混悬液。鼻腔给药可作为传统中药成分黄芩苷治疗脑部疾病一种极具优势的给药途径。

OBJECTIVE To investigate the distribution of nasal baicalin-phospholipid complex in-situ gel in rat blood and brain tissues and to evaluate its brain targeting effect. METHODS After intravenous administration of baicalin-phospholipid solution, in- tranasal administration of baicalin phospholipid complex suspension and in-situ gel, respectively, the concentrations of baicalin in rat plasma and brain tissues were determined by HPLC. RESULTS Compared to intravenous baicalin-phospholipid complex solution,the suspension and in-situ gel produced significant increase of drug distribution in brain tissues. The BTI of insitu gel was higher than that of the suspension,and the olfactory propotion was 88. 8% and 79. 1% ,respectively. The mean residence time （MRT） of the former in- creased nearly 3 times than the latter. CONCLUSION Baicalin-phospholipid complex suspension and in situ gel can improve the brain targeting, for which the in-situ gel is more excellent than the suspension. The result indicates that intranasal administration of baicalin as a treatment for brain diseases has strong competitive advantage.