Aphios
Corporation Granted United States Patent for Drug Delivery
Technique
Reduces Toxicity and Improves Efficacy of Taxol®
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/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
cyclosporin, doxorubicin, daunorubicin, teniposide, micnazole,
and amphotericin can be efficiently maufactured 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 headquartered at 3-E Gill Street, Woburn, Massachusetts
01801, USA, tel: (781) 932-6933, fax: (781) 932-6865, e-mail:
aphios@aol.com. The
Company is 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 http://www.wallstreetinterview.com.
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