Aphios secures subcontract for nanoformulation of super hydrophobic anticancer drug

Several promising natural products being developed as the active pharmaceutical ingredients of investigational drug products have encountered roadblocks that nanotechnology may be able to address. One of these promising anticancer drugs is Brefeldin A (BFA), a cyclic macrolide with a lactone ring.

BFA has demonstrated potent activities in controlling protein trafficking, signal transduction cycles and apoptosis. However, clinical development of this promising anticancer drug has been halted because of the inability to develop an intravenous formulation of this water-insoluble, highly hydrophobic active pharmaceutical ingredient.

The primary goal of this research program is to pair Brefeldin A (BFA) with Aphios’ SuperFluids critical fluid nanosomes (SFS-CFN) technology for intravenous administration to achieve and maintain therapeutic plasma concentrations.

The nanoBFA IV research is being funded via a research subcontract from Leidos Biomedical Research, Inc., prime contractor for the Frederick National Lab, sponsored by the National Cancer Institute.

Dr. Trevor P. Castor, Principal Investigator of the subcontract, states that “Our rationale for pairing BFA with SFS-CFN technology is that BFA is highly hydrophobic and insoluble in water. As such, during the encapsulation process, BFA will be sequestered in the lipid bilayer of phospholipid nanosomes making an aqueous-based nanoformulation of this water-insoluble drug.

"This process is very similar to one that we have developed for Camptothecin (CPT), a highly hydrophobic and water-insoluble lactone, derivatives of which are approved by the FDA for colorectal, cervical, pancreatic and other cancers. Aphios is also developing nanosomes of neat CPT, Camposomes™, to improve efficacy and reduce toxicity of this potent topoisomerase-1 inhibitor for pancreatic and other cancers.”