論文 - 詳細
| RRC ID | 65670 |
|---|---|
| 著者 | Bíró T, Bocsik A, Jurišić Dukovski B, Gróf I, Lovrić J, Csóka I, Deli MA, Aigner Z. |
| タイトル | New Approach in Ocular Drug Delivery: In vitro and ex vivo Investigation of Cyclodextrin-Containing, Mucoadhesive Eye Drop Formulations. |
| ジャーナル | Drug Des Devel Ther |
| Abstract |
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. |
| 巻・号 | 15 |
| ページ | 351-360 |
| 公開日 | 2021-1-1 |
| DOI | 10.2147/DDDT.S264745 |
| PII | 264745 |
| PMID | 33568896 |
| PMC | PMC7868180 |
| MeSH | Animals Cells, Cultured Cyclodextrins / administration & dosage* Drug Compounding Drug Delivery Systems* Female Humans Male Ophthalmic Solutions / administration & dosage* Swine |
| IF | 3.216 |
| リソース情報 | |
| ヒト・動物細胞 | HCE-T(RCB2280) |