Aphios Granted US Patent for Drug Delivery Technique Reduces Toxicity and Improves Efficacy of Taxol
June 02, 1999
Woburn, MA — June 02, 1999 — Aphios Corporation has been granted United States Patent No. 5,776,486 on July 07, 1998. The patent is titled "Method and Apparatus for Making Liposomes containing Hydrophobic Drugs." The patent and certain products developed utilizing this technology are available for licensing.

Hydrophobic drug(s) and liposomal raw materials are first dissolved in supercritical, critical or near-critical fluids with or without cosolvents (SuperFluids™) which are then utilized to form small, uniform liposomes with a high encapsulation efficiency. SuperFluids™ are normally gases which, when compressed, exhibit enhanced solvation, penetration, expansion and disruption properties. These fluids are reverse-engineered to form stable biocompatible aqueous formulations of difficult-to-formulate anti-cancer and anti-viral drugs such as paclitaxel and camptothecin in Aphios' SuperFluids™ CFL (critical fluid liposomal) process.

Paclitaxel is commercially formulated as Taxol® in a castor oil solvent (Cremophor EL) which is quite toxic and can have serious side effects. Taxol®, a unique anti-mitotic agent, has been approved by the FDA for use in ovarian and breast cancers, and is in clinical use for a number of other indications. Taxol® sales have increased from $50 million in 1992 to approximately $1 billion in 1997, compounding at a rate of 85 % per year. Taxol® is a registered trademark of the Bristol-Myers Squibb Company.

SuperFluids™ CFL has been used for the nanoencapsulation of paclitaxel in an aqueous liposomal formulation called Taxosomes™. Independent researchers have shown that 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.

SuperFluids™ CFL has also been used for the nanoencapsulation of camptothecin, a potent and exciting anti-cancer 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. These derivatives are less stable and may not be as effective as neat camptothecin derived from the Chinese tree, Camptotheca acuminata. From in vivo studies, Camposomes™ have been shown to be very effective against lymphomas in nude mice.

Improved drug delivery formulations of hydrophobic drugs such as cyclosporine, doxorubicin, daunorubicin, teniposide, micnazole and amphotericin can be efficiently manufactured utilizing SuperFluids™ CLF in a sterile and scalable manner. SuperFluids™ CLF 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.

Aphios Corporation is a privately held research and development company developing research tools and industrial processes for the improved discovery, manufacturing, delivery and safety of naturally derived and genetically engineered therapeutics for the treatment of cancer, AIDS, and other infectious diseases in a cost-effective manner. The Company is profiled in a recent interview on WallStreetInterview.com.