姜黄素-PLGA纳米粒温敏原位凝胶的制备及其在兔眼房水中的药动学研究  

Study on Preparation of Curcumin-PLGA Nanoparticles Thermosensitive in-situ Gel and Its Pharmacokinetics in Aqueous Humor of Rabbits

作　　者：李林芝 刘梅[2] 常颖 LI Linzhi;LIU Mei;CHANG Ying(Dept.of Geriatrics,Chongqing People’s Hospital,Chongqing 400014,China;Dept.of Pharmacy,Chongqing Hospital of TCM,Chongqing 400021,China)

机构地区：[1]重庆市人民医院老年科,重庆400014 [2]重庆市中医院药剂科,重庆400021

出　　处：《中国药房》2018年第5期640-643,共4页China Pharmacy

摘　　要：目的:制备载姜黄素(CUR)-聚乳酸/羟基乙酸共聚物(PLGA)纳米粒的温敏原位凝胶(CUR-PLGA-GEL),研究其在兔眼房水中的药动学特征。方法:采用改良的乳化-溶剂挥发法制备CUR-PLGA纳米粒,以泊洛沙姆407(P407)和泊洛沙姆188(P188)为凝胶基质,冷溶法制备CUR-PLGA-GEL,高效液相色谱法测定凝胶中CUR水平,并考察其对兔眼的刺激性(5只兔左、右眼自身对照,采用Draize测试进行刺激性评分);10只新西兰白兔随机分为2组,每组5只,左眼分别滴加CUR-PLGA-GEL或CUR混悬液(含CUR 8 mg),分别测定给药前及给药后1、2、4、6、8、10、12、24 h时兔眼房水中CUR的浓度;采用DAS 2.0软件计算药动学参数。结果:成功制备了CUR-PLGA-GEL,其兔眼刺激性评分总分为0分,表明其对兔眼刺激性小。兔眼房水中,CUR-PLGA-GEL的cmax和AUC0-24 h分别是CUR混悬液的2.48和2.71倍。结论:制备的CUR-PLGA-GEL可用于眼部给药,可提高CUR在眼部的利用度。OBJECTIVE:To prepare curcumin(CUR)-Poly(lactic-co-glycolic acid)(PLGA)nanoparticles(CUR-PLGA)thermosensitive in-situ gel(CUR-PLGA-GEL),and to study pharmacokinetic characteristics of it in aqueous humor of rabbits.METHODS:CUR-PLGA was prepared with modified emulsion-solvent evaporation method.CUR-PLGA-GEL was prepared by cold-dissolving method using poloxamer407(P407)and poloxamer 188(P188)as gel matrix.The level of CUR in gel was determined by HPLC,and the irritation of it to rabbit eyes was investigated(self-control of left and right eyes of 5 rabbits were taken,while the Draize test was used to evalvate the irritation).10 New Zealand white rabbits were randomly divided into 2 groups,with 5 rabbits in each group.Left eyes were given CUR-PLGA-GEL and CUR suspension(containing CUR 8 mg),respectively.The concentrations of CUR in aqueous humor of rabbits were determined before medication and 1,2,4,6,8,10,12,24 h after medication.The pharmacokinetic parameters were calculated by using DAS 2.0 software.RESULTS:CUR-PLGA-GEL was successfully prepared and the total score of irritation was 0,which indicated irritative to rabbits.In aqueous humor of rabbits,cmax and AUC0-24 h of CUR-PLGA-GEL were 2.48 and 2.71 fold of CUR suspension.CONCLUSIONS:Prepared CUR-PLGA-GEL can be used for ophthalmic delivery and can improve the utilization of CUR in the eye.

关 键 词：姜黄素 聚乳酸/羟基乙酸共聚物纳米粒 温敏原位凝胶 眼部给药 刺激性 兔 房水 药动学 

分 类 号：R285.5[医药卫生—中药学]