期刊
DRUG DESIGN DEVELOPMENT AND THERAPY
卷 15, 期 -, 页码 351-360出版社
DOVE MEDICAL PRESS LTD
DOI: 10.2147/DDDT.S264745
关键词
prednisolone; cyclodextrin; ocular drug delivery; mucoadhesion; human corneal epithelial cell line; ex vivo cornea model
资金
- Ministry for Innovation and Technology [UNKP-19-3-SZTE-26]
- Campus Mundi Program of Tempus Foundation [EFOP-3.4.2-VEKOP-15-2015-00001]
- University of Zagreb [Z169]
In this study, prednisolone-containing ophthalmic formulations with cyclodextrin-based inclusion complex and a biopolymer were developed to enhance drug permeability and reduce toxicity. Results showed that compared to the conventional benzalkonium-chloride, the novel formulations exhibited lower cytotoxicity and higher drug permeability. These findings suggest the innovative potential and promising application of the new non-toxic ophthalmic formulations.
Background: Optimal transcorneal penetration is necessary for ocular therapy; meanwhile, it is limited by the complex structure and defensive mechanisms of the eye. Antimicrobial stability of topical ophthalmic formulations is especially important. According to previous studies, the mostly used preservative, benzalkonium-chloride is irritative and toxic on corneal epithelial cells; therefore, novel non-toxic, antimicrobial agents are required. In this study, prednisolone-containing ophthalmic formulations were developed with expected optimal permeation without toxic or irritative effects. Methods: The toxicity and permeability of prednisolone-containing eye drops were studied on a human corneal epithelial cell line (HCE-T) and ex vivo cornea model. The lipophilic drug is dissolved by the formation of cyclodextrin inclusion complex. Zinc-containing mucoadhesive biopolymer was applied as an alternative preservative agent, whose toxicity was compared with benzalkonium-chloride. Results: As the results show, benzalkonium-chloride-containing samples were toxic on HCE-T cells. The biopolymer caused no cell damage after the treatment. This was confirmed by immunohistochemistry assay. The in vitro permeability was significantly higher in formulations with prednisolone-cyclodextrin complex compared with suspension formulation. According to the ex vivo permeability study, the biopolymer-containing samples had significantly lower permeability. Conclusion: Considering the mucoadhesive attribute of target formulations, prolonged absorption is expected after application with less frequent administration. It can be stated that the compositions are innovative approaches as novel non-toxic ophthalmic formulations with optimal drug permeability.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据