Ocular Tolerability of Preservative-Free Tafluprost and Latanoprost: in vitro and in vivo Comparative Study
Yoshihiko Esaki1, Atsushi Shimazaki1, Pertti Pellinen2, *
1 Santen Pharmaceutical Co, Ltd, Nara, Japan
2 Santen Oy, Tampere, Finland
Detrimental effects of the preserved prostaglandin analogs (PGAs) have been thoroughly documented in the published literature. The current work studied two preservative-free (PF) prostaglandin eye drops: PF tafluprost and PF latanoprost. The aim of the study was to compare these two PF formulations in vitro for viability of the human corneal epithelial (HCE-T) cells and in vivo for ocular tolerability of the rabbit eye.
Viability of the HCE-T cells was measured by the MTS assay. The SV40-immortalized HCE-T cells were exposed to 100 µL of the drug solutions (at their commercial concentrations) or the culture medium. Ocular irritation was evaluated after repeated instillation of the drug solutions in Japanese white rabbits (Kbl:JW).
A significant loss of HCE-T cell viability was observed in vitro immediately after the exposure to PF latanoprost formulation but not immediately after the exposure to PF tafluprost formulation. Congruently, PF latanoprost induced in vivo more irritation on the rabbit eye than PF tafluprost.
Comparing these two PF formulations in vitro and in vivo, it is considered that ocular tolerability of PF tafluprost is better than PF latanoprost. Taking into account the composition of these two PF PGA formulations, the solubilizing agent macrogolglycerol hydroxystearate 40 (MGHS40) contained in PF latanoprost formulation is a plausible cause for the negative effects.