SYL1001 Targeting TRPV1 Receptor for the Treatment of Ocular Pain associated to Dry Eye Syndrome .
... Results: In vitro and in vivo studies successfully demonstrated that ocular topical administration of SYL1001 was able to reduce TRPV1 levels and ocular pain in New Zealand white rabbits. Moreover, topical administration of SYL1001 prevents ocular pain after pain induction by capsaicin with a similar or higher analgesic effect than the reference analgesic standard. The toxicology experiments performed with SYL1001 by ocular topical route to dogs and rabbits indicated that no side effects were observed during 28-days of treatment. Pharmacokinetic analysis showed that no drug was detected above the detection limit (40 ng/mL) at any time or dose tested.
Conclusions: SYL1001 specifically directed to silence the TRPV1 gene appears to decrease the behavioural response to ocular surface irritation evoked by ocular capsaicin. These channels are involved in the nerve impulse responses to exogenous and endogenous substances mediating inflammation and pain. Toxicology results indicated that SYL1001 did not produce any adverse events related to treatment. SYL1001 has been demonstrated to be safe and efficient in recommended animal models, which suggest this product could be a very good candidate for treatment of ocular pain.