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
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篇名: 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
TITLE:
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。
ABSTRACT: 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.
期刊: 2018年第29卷第5期
作者: 李林芝,刘梅,常颖
AUTHORS: LI Linzhi,LIU Mei,CHANG Ying
关键字: 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
KEYWORDS: Curcumin; Poly (lactic-co-glycolic acid) nanoparticles; Thermosensitive in-situ gel; Ophthalmic delivery; Irritation; Rabbit; Aqueous humor; Pharmacokinetics
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