Sun Jingfen, Zhou Zhengshen
Department of Ophthalmology, Ruijin Hospital, Affiliated to Shanghai Jiao Tong University School of Medicine, Shanghai, People's Republic of China.
Drug Des Devel Ther. 2018 Feb 23;12:383-389. doi: 10.2147/DDDT.S153405. eCollection 2018.
The aim of the study was to develop a sustained ocular delivery of brinzolamide (BLZ) based on gellan gum.
The formulations were characterized for clarity, gelling capacity, rheological studies, pH, drug content, and in vitro drug-release behavior. In vivo rabbit eye irritation test was conducted to evaluate irritation of the BLZ gel drug-delivery system. The prepared BLZ formulations were then investigated in vivo and compared with commercially available BLZ eyedrops with regard to pharmacodynamics.
The results showed that the optimum concentration of gellan gum was 0.25% w/v; the prepared liquid was converted into a flowing gel after the addition of simulated tear fluid. In vitro release profiles showed that the release of BLZ from the in situ gel exhibited sustained characteristics. Draize test results showed that BLZ in situ gels did not stimulate signs of eye tissue activity and were less irritating than BLZ solutions and commercial Azopt.
The results of pharmacodynamics implied that the novel preparation of BLZ in situ gel effectively prolonged the intraocular pressure-lowering effect after administration.
本研究的目的是开发一种基于结冷胶的布林佐胺（BLZ）眼部缓释制剂。
对制剂的澄清度、胶凝能力、流变学研究、pH值、药物含量和体外药物释放行为进行表征。进行体内兔眼刺激性试验以评估BLZ凝胶给药系统的刺激性。然后对制备的BLZ制剂进行体内研究，并在药效学方面与市售的BLZ滴眼液进行比较。
结果表明，结冷胶的最佳浓度为0.25%（w/v）；加入模拟泪液后，制备的液体转变为可流动的凝胶。体外释放曲线表明，BLZ从原位凝胶中的释放具有缓释特性。Draize试验结果表明，BLZ原位凝胶未刺激眼组织活性迹象，且刺激性低于BLZ溶液和市售的Azopt。
药效学结果表明，新型BLZ原位凝胶制剂给药后能有效延长降眼压作用。
