RespireRx Pharmaceuticals Inc. announced that it has filed a provisional patent application describing novel lipid based formulation technology (LFT) that may be used to improve the solubility and bioavailability of poorly soluble drugs, particularly cannabinoids. Low aqueous solubility is a major problem encountered during the formulation development of drug molecules, with an estimated 70% of current drug research pipelines containing such molecules. Because of its recent use in the formulation of mRNA vaccines for COVID-19, LFT has become a focus for formulation research efforts.

ResolutionRx, company's business unit focused on pharmaceutical cannabinoids, has been developing dronabinol (a synthetic form of 9-tetrahydrocannabinol (“THC”)) that acts upon the nervous system's endogenous cannabinoid receptors. Dronabinol was approved in 1985 by the FDA as Marinol® for the treatment of AIDS-related anorexia and later for the treatment of chemotherapy-induced nausea and vomiting. Using the commercial form of dronabinol, company have successfully completed two Phase 2 clinical trials demonstrating significant reductions in the major symptoms of obstructive sleep apnea (OSA).

However, based on these results and those from pharmacokinetic studies, company have concluded that expansion of dronabinol's use into OSA and other therapeutic indications will require new, improved formulations. As it is commercially sold, dronabinol is formulated as a sesame oil emulsion in a soft gelatin capsule that suffers from poor and highly variable absorption, low blood levels resulting from rapid and extensive (approximately 80%) first pass liver metabolism, as well as a relatively brief half-life (approximately 2 – 3 hours) requiring high doses in order to achieve sustained, therapeutic blood levels for 4 hours or longer. In order to circumvent these problems, company have designated certain important properties around which company have created a number of lipid nanoparticle (LNP) formulations of dronabinol, three (3) of which (i) display appropriate water solubility and dissolution to improve absorption, (ii) nano-particle size and resistance to stomach acid conditions in order to reduce first pass liver metabolism and achieve higher and longer blood levels, as well as (iii) stability and ease of manufacturing to support commercial scale.

Pending additional financing (availability of which cannot be assured), company plan to test these formulations in animal and human pharmacokinetic (PK) and pharmacodynamic (PD) studies. Company believe that the development of a novel, proprietary formulation of dronabinol would not require significantly longer time to market entry compared to what would be required if company was to use the currently available soft gel capsule technology.