Preparation and characterization of a hydrogel carrier to deliver gatifloxacin and its application as a therapeutic contact lens for bacterial keratitis therapy.
A soft and biocompatible hydrogel exhibiting a higher loading and the sustained release of gatifloxacin (GFLX) was developed as the potential matrix to fabricate a therapeutic contact lens for curing bacterial keratitis. 2-hydroxyethyl methacrylate (HEMA) and five other kinds of vinyl monomers with different side groups were used as co-monomers. Copolymerization took place in a cornea shaped mould via the gradient temperature-elevating method. The results of drug loading and in vitro release experiments showed that P(HEMA-co-MAA) achieved the highest drug loading of 11.78±0.77 µg mg(-1) among the obtained hydrogels, as well as a slow release. In addition, its physical properties and cytocompatibility were also proved suitable and safe for wearing on the eye surface. In animal experiments, a rat model of bacterial keratitis was established and employed to evaluate the clinical results of certain treatments employing obtained hydrogels; saline and GFLX eye drops were used as negative and positive controls, respectively. Corneal abscess and opacity caused by epithelial erosion and stromal ulceration were almost healed after wearing the drug loaded P(HEMA-co-MAA) hydrogel for 48 h. Its excellent antibacterial effect was also confirmed by testing the bacterial activity in tear extraction via the streak line method.
Institute of Biomedical Engineering, Jinan University, Guangzhou, 510632, People's Republic of China. Key Laboratory of Biomaterials & Protein Research of Guangdong Higher Education Institutes, Jinan University, Guangzhou, 510632, People's Republic of China.
Yunfeng
Y
Shi
Hongling
H
Lv
Yeyun
Y
Fu
Qingjun
Q
Lu
Jingxiang
J
Zhong
Dong
D
Ma
Yuexin
Y
Huang
Wei
W
Xue
D000818:Animals; D000900:Anti-Bacterial Agents / Q000008:administration & dosage*; D001424:Bacterial Infections / Q000188:drug therapy* / Q000382:microbiology; D002460:Cell Line; D003261:Contact Lenses; D004337:Drug Carriers; D024841:Fluoroquinolones / Q000008:administration & dosage*; D000077734:Gatifloxacin; D006801:Humans; D020100:Hydrogels / Q000737:chemistry*; D007634:Keratitis / Q000188:drug therapy* / Q000382:microbiology; D008689:Methacrylates / Q000737:chemistry; D011108:Polymers / Q000737:chemistry; D051381:Rats; D017207:Rats, Sprague-Dawley; D013997:Time Factors
D000900:Anti-Bacterial Agents; D004337:Drug Carriers; D024841:Fluoroquinolones; D020100:Hydrogels; D008689:Methacrylates; D011108:Polymers; C005044:hydroxyethyl methacrylate; D000077734:Gatifloxacin