Preparation，Characterization and in vitro Evaluation of PTMAc-PEG-PTMAc Hydrogel for Ocular Drug Carrier of Pirfenidone
- VernacularTitle:吡非尼酮药物缓释载体PTMAc-PEG-PTMAc水凝胶制备与体外实验
- Author:
Wei PENG
1
;
Yang-fan YANG
1
;
Xian-chai LIN
1
;
Tao WANG
2
;
Da-ping QUAN
2
;
Kai-li WU
1
;
Min-bin YU
1
Author Information
1. Department of Glaucoma，Zhongshan Ophthalmic Center，SunYat-sen University，Guangzhou 510060
2. School of Chemistry，SunYat-senUniversity，Guangzhou 510275
- Publication Type:Journal Article
- From:
Journal of Sun Yat-sen University(Medical Sciences)
2019;40(2):219-227
- CountryChina
- Language:Chinese
-
Abstract:
【Objective】To form a new PTMAc- PEG- PTMAc triblock（PPP）copolymerhydrogel and to evaluate its sustained released performance and antiproliferative effects as an ocular drug carrier of Pirfenidone（PFD）【Methods】One type triblockcopolymers PPP hydrogel was chosen. The morphology of the material was evaluated by scanning electron microscopy（SEM）. The swelling properties of the PPP hydrogel was analyzed in PBS solution（37 ℃ ，pH 7.4）. The in vitro drug release of the pirfenidone loaded hydrogels were evaluated with non-dialysis method and the curves of drug release were drawed. We evaluated the adhesion，survival of human Tenon′s capsule fibroblasts（HTF）around hydrogels. The cell cytotoxicity of hydrogels and antiproliferative effects were evaluated through CCK-8 assay.【Results】The hydrogel has stable gelation conditions. The swelling rate decreased by increasing hydrogel concentration.The SEM images indicated the fibrous and porous structure. We also observed that the encapsulated pirfenidone were sustained released from hydrogels with an initial burst release at early stage（within 4 d）and then the release rate were declined for all hydrogels during the following 14 d. The PPP hydrogel can inhibit cell adhesion. The cell viability in hydrogels at four time point（24，48，72 and 96 h）were 85.7% ，93.0% ，82.0% ，81.6%. The inhibition rate of drug loaded hydrogel with two drug concentration（1 mg/mL or 2 mg/mL）are 25.8%，21.8%，55.4%，25.6%；44.6%，35.9%，55.5%，31.4%. While that of drug solution are 28.9% ，29.7% ，7.8% ，7.7%. The suppressive effects of the PFD loaded hydrogels on HTF proliferation followed a dose-dependent fashion and time-dependent fashion.【Conclusions】Such biocompatible copolymers hydrogel can be effectively used as an drug sustain released system. It can induce significant inhibition of HTF proliferation. With equal amount of drug，the inhibition effect of drug loaded gel was longer than that of drug solution.
