Study on Preparation of Curcumin-PLGA Nanoparticles Thermosensitive in-situ Gel and Its Pharmacokinetics in Aqueous Humor of Rabbits
10.6039/j.issn.1001-0408.2018.05.16
- VernacularTitle: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
- Author:
Linzhi LI
1
;
Mei LIU
;
Ying CHANG
Author Information
1. 重庆市人民医院老年科
- Keywords:
Curcumin;
Poly (lactic-co-glycolic acid) nanoparticles;
Thermosensitive in-situ gel;
Ophthalmic delivery;
Irritation;
Rabbit;
Aqueous humor;
Pharmacokinetics
- From:
China Pharmacy
2018;29(5):640-643
- CountryChina
- Language:Chinese
-
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.
