【作者】 吴祥根； 辛萌； 杨丽娜； 史伟云；

【Author】 WU Xiang-gen, XIN Meng, YANG Li-na, SHI Wei-yun (State Key Laboratory Cultivation Base, Shandong Provincial Key Laboratory of Ophthalmology, Shandong Eye Institute, Qingdao,266071, China)

【机构】 山东省眼科研究所； 山东省眼科学重点实验室-省部共建国家重点实验室培育基地；

【摘要】 目的评价白芨多糖促进角膜对药物的吸收作用及其在滴眼液中应用的可行性。方法采用角膜上皮细胞毒性实验评价白芨多糖的细胞毒性,Fern试验考察白芨多糖与泪液的相似度,兔滴眼后测定眼部药物动力学特性和相对生物利用度评价白芨多糖的缓释性和促进角膜对药物的吸收作用。结果白芨多糖不仅没有表现出角膜上皮细胞毒性,还能促进角膜上皮细胞的生长,有利于感染后的角膜修复,Fern试验结果表明白芨多糖符合泪液特性,适合于滴眼液中应用。药物动力学研究表明左氧白芨滴眼液组房水和角膜中药物质量浓度曲线下面积(AUC0-240)分别是对照药物可乐必妥组的1.78倍、1.37倍,这说明白芨多糖显著促进角膜对药物的吸收。结论白芨多糖将是一种很有眼科应用前景的"活性"滴眼液辅料。更多还原

【Abstract】 OBJECT The present study was to evaluate a novel mucoadhesive polymer extracted from Bletilla striata to be used for ocular delivery 0.5% levofloxacin in rabbits. METHOD The bletilla striata polysaccharides(BsP) was subjected to the cell cytotoxicity and ferning test. The pharmacokinetics and bioavailability of topically applied 0.5% levofloxacin-bletilla striata polysaccharides eye drops(0.5% levofloxacin-BsP eye drops)was investigated and compared with the 0.5% levofloxacin eye drops (Cravit). RESULTS It showed that BsP markedly increased the proliferative efficacy of HCECs. And the ferning test showed that BsP exhibited optimal performance as a tear fluid. The polysaccharides significantly increased the intra-aqueous penetration and cornea accumulation in rabbits. CONCLUSION The BsP appears to be a promising candidate as a vehicle for the topical ophthalmic drug delivery.更多还原