Opportunities & Challenges
While the promise of cannabinoids is unparalleled, they will become an increasingly researched group of compounds giving birth to several medicines, yet there are key issues that need to be addressed before we see their therapeutic potential fully realized.
The two main challenges are:
- Delivery and bioavailability
Cannabinoids as a class are extremely sensitive to acidic environments and degrade quickly in the stomach. In addition, they are further degraded in the liver, thereby making oral delivery impractical at present. Even though Epidiolex is expected to be approved for the treatment of Dravet Syndrome, its bioavailability is poor and would require large cultivations of the plant to generate enough drug for marketing. The best bioavailability is seen through inhalation – as smoke of the original cannabis plant – but that has significant associated negative side-effects related to smoke inhalation.
“Cannabinoids are a poorly water-soluble class of compounds and many degrade as pure solids. Hence formulating them and delivering them in a manner that provides significant bioavailability is a key challenge.”
A few industry players are developing Cannabinoid patches and gels to deliver these compounds transdermally. However, these transdermal delivery modalities have limitations. In contrast, SGN’s MNP Platform is ideal to deliver these molecules as nanoemulsions and we have developed several nanoformulations that deliver Cannabinoids through skin, ophthalmic, oral and pulmonary routes. We believe we have validated technology that will be suitable to deliver these molecules to harness their significantly large medicinal potential.
Our key areas of focus for NanoCannabinoids will be:
- TransNanoCannis: Transdermal delivery for pain relief and anti-inflammatory indications: Some cannabinoids (THC) are powerful anti-inflammatory agents with 2 times the power of steroids and 20 times that of aspirin (Russo, E.B., 2011, British Journal of Pharmacology, 2011, 163 1344-1364; Evans F, 1991, Planta Med, 57: 560-567). MNP Cannabinoid formulations entail individual as well as multiple synergistic cannabinoids in one formulation. These are designed to provide local as well as systemic therapeutic effects and are ideal transdermal formulations because of excellent skin penetration and spreading capabilities. Target indications will likely include Rheumatoid arthritis, pain, psoriasis, eczema. We expect to file our first regulatory filing for Phase 1, in Australia, by mid-2020.
- OphthaNanoCannis: For Ophthalmic Indications: We have developed traditional MNP formulations for ophthalmic indications including MNP Nanoyclosporine for dry eye, which is currently marketed in India and undergoing Phase II testing vs. RestasisTM . We have applied the same formulation technology and developed MNP Cannabinoids for potential treatment of several ophthalmic indications. We expect to initiate Phase I studies in Australia around mid-2020.
- CNSNanoCannis: Delivery of Cannabinoids to the brain: Delivering Cannabinoids across the blood-brain barrier remains a key hurdle. We are currently working on developing formulations that cross the blood-brain barrier in a significantly superior manner versus conventional non-nano formulations with the intention of developing of Cannabinoids to treat neural indications such as Alzheimer’s, and other disorders. Given the demonstrated benefits of oral MNP formulations in improving bioavailability, we believe a great opportunity lies in developing oral and intra-nasal nano-formulations of cannabinoids that have (1) enhanced bioavailability compared to current therapeutics such as Epidolex and (2) ability to readily cross the blood-brain barrier. We have been awarded (in collaboration with Professor Sanchez-Ramos, USF, Tampa – see bio in Advisory Board) a Florida I4 HiTech Grant (by the State of Florida) to study “Nanoformulations of Cannabinoids for Nose to Brain Delivery).