Skye Bioscience Reports Enhanced IOP-Lowering of SBI-100 Formulation

Skye Bioscience announced that the peer-reviewed journal International Journal of Pharmaceutics published preclinical data demonstrating stronger and longer-lasting reduction of IOP when Skye’s proprietary molecule, SBI-100, is formulated as a nanoemulsion containing the mucoadhesive agent Carbopol 940.

The results of the research were published March 2022 in a paper, “Impact of mucoadhesive agent inclusion on the intraocular pressure lowering profile of Δ9-tetrahydrocannabinol-valine-hemisuccinate loaded nanoemulsions in New Zealand white rabbits,” authored by C. Sweeney et al. from the University of Mississippi (UM).

Skye, in collaboration with UM, previously published preclinical data demonstrating SBI-100 formulated as a nanoemulsion (THC-VHS-NE) achieved greater reduction of IOP in nonpigmented rabbits than both latanoprost and timilol,¹ the current first and second line treatments for glaucoma, respectively. The current study was undertaken to determine if the inclusion of a mucoadhesive agent could prolong the intensity and duration of action of the THC-VHS-NE formulation through increased residence time or penetration, or both, to potentially achieve once- or twice-per-day dosing.

In this study sponsored by Skye, researchers at UM compared the reduction of IOP in normotensive rabbits with a single treatment of THC-VHS-NEC (SBI-100 formulated as a nanoemulsion with Carbopol 940) compared to latanoprost, the commercial standard of care; THC-NEC (native THC formulated as a nanoemulsion with Carbopol 940); and THC-VHS-NE (SBI-100 formulated as just a nanoemulsion). When comparing each treatment group, THC-VHS-NEC, Skye’s SBI-100 Opthalmic Emulsion, demonstrated the greatest intensity and duration of IOP-lowering.

“Skye has been working aggressively to optimize a formulation of SBI-100 to advance toward a first in-human study, which is planned to start this quarter. We previously reported strong preclinical results that highlighted the superior IOP-lowering of our unique molecule formulated as just a nanoemulsion compared to other established commercial glaucoma drugs. This further evolution of our formulation, generating even more robust results, gives us strong conviction as we step into the clinic with SBI-100 Ophthalmic Emulsion,” said Punit Dhillon, CEO and chair of Skye.

In comparison to THC-VHS-NE, THC-NEC and commercial latanoprost, THC-VHS-NEC (SBI-100 Ophthalmic Emulsion) exhibited a prolonged duration of action. THC-NEC and THC-VHS-NE formulations respectively produced an average maximum drop in IOP of 3.7 mmHg at 60 minutes and 4.8 mmHg at 150 minutes, while the IOP-lowering effect lasted for 240 and 360 minutes, respectively, in the treated eye. In contrast, SBI-100 Ophthalmic Emulsion lowered IOP by 4.5 mmHg at 60 minutes and maintained this drop for at least 480 minutes in the treated eye.

A significant difference (P<0.05) in IOP-lowering was also observed between SBI-100 Ophthalmic Emulsion and commercial latanoprost ophthalmic solution. The average maximum drop in IOP with SBI-100 Ophthalmic Emulsion (THC-VHS-NEC) of 4.5 mmHg at 60 minutes was almost twice that obtained with commercial latanoprost ophthalmic solution (2.3 mmHg) at 60 minutes. Moreover, latanoprost maintained IOP 10% below baseline for 360 minutes, whereas SBI-100 Ophthalmic Emulsion maintained the IOP-lowering effect for at least 480 minutes (p < 0.05).

1. Sweeney, C, Dudhipala, N, Thakkar, R, et al. Effect of surfactant concentration and sterilization process on intraocular pressure–lowering activity of Δ9-tetrahydrocannabinol-valine-hemisuccinate (NB1111) nanoemulsions. Drug Deliv. and Transl. Res. 11, 2096–2107 (2021). https://doi.org/10.1007/s13346-020-00871-9
** SBI-100 has previously also been referred to as THCVHS and/or NB1111