Aphios
Corporation Granted European Patent for Nanoencapsulation
of Cancer Drugs
December
11, 2002
— 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™
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, 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 (www.aphios.com)
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.
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