Aphios Corporation Granted European Patent for Nanoencapsulation of Cancer Drugs
December 11, 2002
Woburn, MA — Aphios Corporation has been granted European Patent No. 0792143 on September 04, 2002. The patent is entitled "Methods for Making Liposomes containing Hydrophobic Drugs."

The patented technology can be utilized to form stable biocompatible aqueous formulations of poorly soluble anticancer and antiviral drugs such as paclitaxel and camptothecin. The poorly soluble (hydrophobic drug) and phospholipid are first dissolved in supercritical, critical or near-critical fluids with/without cosolvents (SuperFluids™) which are then utilized to form small, uniform liposomes (nanosomes) with a high encapsulation efficiency.

The process has been used for the nanoencapsulation of paclitaxel in a formulation called Taxosomes™. Taxosomes™ are much less toxic in vitro than Taxol®, while being twice as effective as Taxol® from in vivo studies of nude mice with breast cancer xenografts. Taxosomes™ will lead to: (i) enhanced therapeutic efficacy; (ii) elimination of pre-medication to counteract castor oil; (iii) reduction of drug toxicity side-effects; (iv) prolonged circulation time and therapeutic effect; and (v) improved quality of life.

The process has also been used for the nanoencapsulation of camptothecin, a potent and exciting anticancer agent, in a stable aqueous liposomal formulation called Camposomes™. Water soluble derivatives of camptothecin, a unique topoisomerase 1 inhibitor, have recently been approved by the FDA for use in colorectal cancer. Camposomes™ has been shown to be very effective against lymphomas in nude mice.

Improved drug delivery formulations of hydrophobic drugs such as cyclosporine, doxorubicin, daunorubicin, teniposide and amphotericin can be efficiently manufactured utilizing the patented process in a sterile and scalable manner. The process can also be utilized for the nanoencapsulation of hydrophilic drugs and proteins.

Research leading to the development of this technology was partially funded by Small Business Innovative Research (SBIR) grants from the National Science Foundation and the National Cancer Institute, National Institutes of Health, USA.

Aphios Corporation is a biopharmaceutical company that is developing enhanced natural therapeutics for health maintenance and the treatment of human diseases with a focus on infectious diseases, cancer and quality-of-life medicines. Aphios' product pipeline includes therapeutics from medicinal plants and marine organisms, and improved drug delivery formulations of small anticancer molecules and large protein macromolecules that are crucial to the functioning of the human genome.