Abstract
Purpose :
Nepafenac (NPF) 0.3% is available only as a water suspension due to the lipophilicity. NPF viscous suspension induces blurred vision, eyelids sedimentation and lacrimation; moreover, the presence of the preservative exerts a certain cytotoxicity. Purpose of the study was the development of a platform able to solubilize and stabilize 0.3% NPF in a preservative-free aqueous formulation (MDV1604- WO2020148645A1).
Methods :
NPF (0.3%) was solubilized in low content cyclodextrin aqueous solution in presence of Hyaluronic Acid (HA 0.25%) and Polyvinyl Alcohol (PVA 1%). MDV1604 shelf-life was evaluated according to International Conference of Harmonization (ICH) guidelines. Chemical stability and degradation products were monitored using validated HPLC methods. The ocular viability test of MDV1604 was conducted in comparison with NEVANAC (Alcon) and their respective vehicles on the human corneal epithelial cell line HCE-2. Cytotoxicity was determined 24h after exposure to the test compounds using MTT assays.
Results :
The stability study, conducted at 25°C (12 months) and 2-8°C (24 months), showed no significant changes for any chemical-physical parameter of MDV1604. The degradation products, all less than 1%, were fully characterized. The results of the viability tests showed a viability of 75% for the preservative-free MDV1604, compared to 35% for NEVANAC.
Conclusions :
MDV1604, an eye drops in which NPF is formulated as a clear solution, showed an improved profile in terms of safety versus commercial 0.3% NPF. Moreover, MDV1604 is physically and chemically stable.
This abstract was presented at the 2023 ARVO Annual Meeting, held in New Orleans, LA, April 23-27, 2023.