PharmAust Limited (ASX:PAA) says its monepantel (MPL) reformulation project has continued to achieve a number of milestones.
The company previously announced the appointment of BRI Pharmaceutical Research to reformulate its lead compound MPL.
Its key goals are to address the bitter taste and low concentrations of drug delivered by the current formulation. The reformulation initiative also aims to improve its oral bioavailability - the amount of drug absorbed from the small intestine into the body.
PharmAust said BRI is assessing three different formulations:
Micronisation: Uses a milling technique to reduce particle size, which can improve the rate of drug absorption into the body. "BRI has successfully milled MPL down to an average particle size of 1µm, which is within the target range. Micronisation can potentially deliver up to 30 times more drug," said the company.
Amorphous Solid Dispersion (ASD): "Initial studies by BRI have confirmed MPL is amenable to ASD formulation. Latest results suggest this approach could deliver up to 20 times more drug than the current formulation using the same size capsules."
Self-Emulsifying Drug Delivery Systems (SEDDS): An oily emulsion-based formulation that can significantly improve the bioavailability of drugs, such as MPL, which are poorly soluble in water. "BRI has shown this approach can deliver six times more drug than the current formulation."
On taste, BRI has not observed unpleasant odours with any of the formulations tested so far, said PharmAust. "Moreover, taste tests conducted at PharmAust using pure MPL noted only a mild bitterness which BRI expects can be addressed with masking and flavouring agents to improve palatability."
It said next steps include continuing further optimisation of each formulation method. BRI expects to begin bioavailability studies in animal models mid-November.