|Category||Life Sciences and Biotechnology|
|Keywords||NAFLD, NASH, Diabetes, Metabolic Syndrome|
|Current development stage||For Pharmaceutical development: TRL4 – PoC&Safety of candidate device or system is demonstrated in a defined lab or animal model|
- The endocannabinoid (eCB) system is involved in the development of obesity and its related comorbidities, specifically NAFLD. eCBs, via activation of the cannabinoid type-1 receptors (CB1Rs) in the liver, increase hepatic glucose production, insulin resistance and de novo lipogenesis, and decrease fatty acid oxidation.
- Accordingly, chronic CB1R blockers improve these parameters both in rodents and humans; however, due to their neuropsychiatric side effects, they are no longer available for clinical use.
- Here, we introduce a novel drug delivery system for peripheralization of a known (previously abandoned) CB1R blocker, for the treatment of NAFLD. Targeting hepatic CB1Rs specifically by Rimonabant encapsulated in nanoparticles (Rimo-NP) can offer a treatment for fatty liver disease.
- This breakthrough technology combines high efficacy with safety of the proposed NPs-encapsulated CB1R blockers.
- We demonstrated the therapeutic value of Rimo-NPs in a rodent model of obesity/metabolic syndrome, and showed:
- An effective delivery of a water insoluble drug (i.e., rimonabant) at a high dose to the liver
- Protecting the drug from the hostile environment
- Controlled delivery and targeting of rimonabant to the liver
- Reducing its toxic centrally mediated side effects
- Efficacy in reversing NAFLD, dyslipidemia, and insulin resistance in mice
- NANOFLD aims to promote the clinical development and testing of our novel methodology for peripheralization of the CB1R blocker, Rimonabant Nanoparticles (Rimo-NP), for the treatment of NAFLD (Fig. 1).
- Rimo-NPs are expected to be the first drug to safely and effectively address the need of NAFLD therapy and preventing liver-related complications.
Provisional patent application #63/202,554 was submitted