In this study, prednisolone-containing ophthalmic formulations were developed with expected optimal permeation without toxic or irritative effects.
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 using HPBCD and HPGCD. Zinc-containing mucoadhesive biopolymer (Zn hyaluronate and Zn gluconate) was applied as an alternative preservative agent, whose toxicity was compared with benzalkonium-chloride.
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.
Considering the mucoadhesive attribute of target formulations, prolonged absorption is expected after application with less frequent administration.
Bíró T, Bocsik A, Jurišić Dukovski B, Gróf I, Lovrić J, Csóka I, Deli MA, Aigner Z NEW Approach in Ocular Drug Delivery: In vitro and ex vivo Investigation of Cyclodextrin-Containing, Mucoadhesive Eye Drop Formulations. Drug Design, Development and Therapy 2021, 15, 351—360