Newsletter
Volume 2, Number 1
January 2007
Newsletter Volume 2, Number 1
January 2007
Page 2
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Phospholipid Research Center news
Founding of the Phospholipid Research Center
Scientific exchange
Access to scientific compositons
Newsletter
Member fees for conferences and workshops
Procurement of analytical services
The Phospholipid Research Center activities extends
the possible utilization and physiological significance of
phospholipids of all kinds (i.e. natural, hydrogenated,
synthetic, and modified phospholipids), and combined
products of phospholipids as excipients and active
ingredients in pharmaceuticals.
Scientific Board
The Phospholipid Research Center was founded as a
non-profit organisation at September 11th 2006 by
famous international scientists and the companies
Lipoid GmbH (Ludwigshafen, Germany) and
Phospholipid GmbH (Köln, Germany).
Dr. Herbert Rebmann (Neustadt, Germany) was
elected as Chairman and Mr. Armin Wendel (Köln,
Germany) as his Deputy.
Prof. Dr. Christel Müller-Goymann
Prof. Dr. Alfred Blume
Prof. Dr. Gert Fricker
Prof. Dr. Om Parkash Katare
Dr. Frank Martin
Dr. Ralf-Olaf Quinkert
Prof. Dr. Kun Wang
The Phospholipid Research Center is located in the
technology park of Heidelberg, on the campus of the
famous Ruprecht-Karls-University of Heidelberg.
The Scientific Board will ensure the scientific expertise
of the Phospholipid Research Center. In 2007 the first
meeting of the Scientific Board will be held at January
29th.
The Phospholipid Research Center will intend to
promote and provide a foundation for the use of
phospholipids in pharmaceutics. Thus, information and
assistance to scientists and practitioners will be
provided by associates and external advisors of the
Phospholipid Research Center, either free of any
charges or at a cost.
Following scientists are the members of the Scientific
Board:
Phospholipid Reviews
The Phospholipid Research Center creates summaries
of the available knowledge of the different areas of
phospholipid research. Based on these reviews open
questions and work on defined topics will be defined.
Membership Benefits
We are interested in the following themes:
The benefits of a membership in the Phospholipid
Research Center are:
Phospholipids and immune system; phospholipids
in vaccines
Oral application of liposomes
Toxicity of lecithins and phospholipids
_____________________________________________________________________________________________________________________
Phospholipid
Im Neuenheimer Feld 582
Phone +49 (0) 6221 - 5888360
Forschungszentrum / Research Center
D-69120 Heidelberg
Fax
+49 (0) 6221 - 6515665
Heidelberg
www.phospholipids.net
Newsletter Volume 2, Number 1
January 2007
Page 3
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Absorption of phospholipids
Phospholipids in the enhancement of drug
absorption
Analytical methods for the quantification of
phospholipids
development of novel therapeutics for the
treatment of cancer.
The Phospholipid Research Center is now looking for
collaborators who will compose reviews of these topics
after an exhaustive literature research.
Time and effort will be compensated in a manner we
have to agree with the authors. We wish to publish the
resulting compositions in the name of the Phospholipid
Research Center with mention of the author.
If you are interested in writing such a review please
contact Dr. Schaffer:
e-mail:
phone:
[email protected]
+49 6221 588 83 60
Industry news
D-Pharm grants an exclusive license for DPb99 in acute stroke in South Korea to Yungjin
Pharmaceutical Company Ltd.
D-Pharm announced that it has granted Yungjin
Pharmaceutical Company Ltd. an exclusive license
to develop, register and market DP-b99 in South
Korea for treatment of patients with acute stroke.
Biomira announces acquisition of ProIX
Pharmaceuticals.
Biomira Inc. announced that it has acquired ProIX
Pharmaceuticals Corporation, a privately-held
biopharmaceutical company focused on the
IDM Pharma submits new drug application to
the FDA for JunovanTM (mifamuride) in the
treatment of osteosarcoma.
IDM Pharma has submitted an electronic New
Drug Application to the U. S. FDA for JunovanTM,
requesting approval for its use in the treatment of
newly diagnosed respectable high grade
osteosarcoma patients following surgical resection
in combination with multiple agent chemotherapy.
JunovanTM is a liposome encapsulated, fully
synthetic derivative of the muramyl dipeptide
European regulatory authority recommends
orphan drug designation for MediGene´s drug
candidate EndoTAG-1.
The biotech company MediGene AG announced
that the European Medicines Agency (EMEA) has
recommended granting of orphan drug designation
for MediGene´s drug candidate EndoTAG-1 in the
indication of pancreatic cancer.
MediGene´s EndoTAG technology aims at
“starving out” tumors and consists of a therapeutic
substance embedded in a positively charged
liposomal carrier.
Celsion obtains from Valentis exclusive rights
to pegylation patents for use with heat
activated liposomes.
Celsion Corporation announced that it has aquired
exclusive worldwide rights for use of pegylation
technology with its heat activated liposome
technology.
_____________________________________________________________________________________________________________________
Phospholipid
Im Neuenheimer Feld 582
Phone +49 (0) 6221 - 5888360
Forschungszentrum / Research Center
D-69120 Heidelberg
Fax
+49 (0) 6221 - 6515665
Heidelberg
www.phospholipids.net
Newsletter Volume 2, Number 1
January 2007
Page 4
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Endovasc announces completion of LC/MS
assay by ABC Laboratories for Phase III trial of
Liprostin.
Endovasc Inc. announced that Analytical BioChemical Laboratories Inc. (ABC) has developed a
high sensitive High Performance Liquid
Chromatography / Mass spectrophotometric assay
(LC/MS) to detect prostaglandin E-1 (PEG-1) in the
serum of patients treated with Liprostin.
Endovasc´s Liprostin is a liposome-encapsulated
form of prostaglandin E-1 which is known to be a
potent vasodilator and platelet inhibitor as well as
an anti-inflammatory and anti-thrombotic agent.
Inex Pharmaceutical Corporation announced that
its partner Hana Biosciences has enrolled the first
patient in a phase I human clinical trial evaluating
the safety, tolerability and preliminary efficacy of
INX-0125 (sphingosomal vinorelbine) as a
treatment for advanced solid tumors.
Commencement of patient dosing for this trial
triggers US$ 1.0 million milestone payment from
Hana to INEX.
Biomira receives special protocol assessment
from the FDA for phase III trial of Stimuvax for
non-small cell lung cancer.
Biomira Inc. announced that it has reached an
agreement with the U. S. FDA on a Special
Protocol Assessment (SPA) for the planned phase
III clinical trial of Stimuvax for the treatment of nonsmall cell lung cancer. The SPA agreement
between Biomira and FDA concerns the design of
the phase III trial and outlines definitive clinical
objectives and data analyses considered
necessary to support regulatory approval of
Stimuvax. The trial will be conducted by Merck
KGaA under terms of licensing agreement with
Biomira.
IDEA AG receives approvable letter from
Swissmedic for IDEA-033, a novel carrierbased, targeted analgesic, for the treatment of
signs and symptoms of osteoarthritis.
IDEA AG announced that it had received an
approvable letter from the Swiss regulatory agency
(Swissmedic) for the carrier-based, targeted
analgesic IDEA-033 for the treatment of signs and
symptoms of osteoarthritis. The positive decision
requires no further toxicological or clinical studies,
and was based on an extensive proprietary data
Oxygenix, a blood substitute marker, expands
into Ontario.
Oxygenix, a Japan-based biotechnology company,
has recognized that Ontario may hold the key to its
future growth. In 2005 Oxygenix established a
branch office in the MaRS building, in Toronto´s
Discovery District. Last year Oxygenix announced
that they are expanding operations in Ontario.
Oxygenix is also looking for new research
partnerships based on its proprietary liposome
technology, which led to the development of
Oxygen carrier, an artificial red cell.
Endovasc announces completion of Liprostin
manufacturing for phase IIIa trial.
Encovasc announced that PYRAMID Laboratories
Inc. has completet the cGMP manufacturing of
Liprostin for the company´s proposed phase IIIa
clinical trial for patients suffering from Intermittent
Claudication.
Commencement of INX-0125 phase I clinical
trial triggers US$ 1.0 million milestone payment
to INEX.
_____________________________________________________________________________________________________________________
Phospholipid
Im Neuenheimer Feld 582
Phone +49 (0) 6221 - 5888360
Forschungszentrum / Research Center
D-69120 Heidelberg
Fax
+49 (0) 6221 - 6515665
Heidelberg
www.phospholipids.net
Newsletter Volume 2, Number 1
January 2007
Page 5
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2362-2367
Core/shell nanoparticles with lipid core, were
prepared and characterized as a sustained
delivery system for protein. The lipid core is
composed of protein-loaded lecithin and the core
shell is composed of Pluronics. Cryo-TEM and a
particle size analyser were used to observe the
formation of stabilized core/shell nanoparicles.
package including the results from long-term
toxicity and Ph I and Ph II clinical studies.
Literature report
A calorimetric study of
dimyristoylphosphatidylcholine phase
transitions and steroid-liposome interactions
for liposomes prepared by thin film and
proliposome methods
Elhissi, A.M.A. et al., Int. J. Pharm. 2006, 320(1-2)
124-130
Using high sensitivity differential scanning
calorimetry (HSDSC), the phase transitions of
dimyristoylphosphatidylcholine (DMPC) liposomal
bilayers and their interaction with the model steroid
beclometasone dipropionate (BDP) were found to
be dependent on the method of liposome
preparation.
Influence of rapeseed phospholipids on
ibuprofen dissolution from solid dispersions
Sosada M., Gorecki M., Pasker B., Pharmazie
2006, 6(8) 677-680
The dissolution profiles of ibuprofen (IB) from solid
dispersions prepared by the solvent evaporation
method, containing the rapeseed lecithin ethanol
soluble fraction (LESF) or rapeseed
Phosphatidylcholine (RPC) have been determined.
Dissolution studies showed that the initial
dissolution rate within the first 5 min and the
maximum percentage of dissolved IB of IB/LESF
were double of those in IB RPC.
Deformable liposomes as topical formulations
containing α-tocopherol
Gallarate M. et al., Journal of Dispersion Science
and Technology, 2006, 27, 703-713
Several deformable liposomes were formulated
using hydrogenated soya lecithin.
Molecular packing in 1-hexanol-DMPC bilayers
studied by molecular dynamics simulation
Pedersen U. R., Peters G. H., Westh P. Biophys
Chem. 2007, 125(1), 104-111
The structure and molecular packing density of a
“mismatched” solute, 1-hexanol, in lipid
membranes of dimyristoylphosphatidylcholine
(DMPC) was studied by molecular dynamics
simulations.
Measurement of Phosphatidylcholine
hydroperoxides in solution and in intact
membranes by the ferric-xylenol orange assay
Fukuzawa K. et al., Anal. Biochem. 2006, 359 (1),
18-25
Formation of a colored complex between ferric iron
and xylenol orange has been used for the
determination of peroxides.
Core/shell nanoparticles with lecithin lipid
cores for protein delivery
Keun Sang Oh et al., Biomacromolecules 2006, 7,
_____________________________________________________________________________________________________________________
Phospholipid
Im Neuenheimer Feld 582
Phone +49 (0) 6221 - 5888360
Forschungszentrum / Research Center
D-69120 Heidelberg
Fax
+49 (0) 6221 - 6515665
Heidelberg
www.phospholipids.net
Newsletter Volume 2, Number 1
January 2007
Page 6
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US Pat. Appl. 2006023596; October 19, 2006
Bracco Imaging S.p.A.
Contrast enhanced x-ray phase imaging
The invention refers to methods of PhaseSensitive-X-ray imaging wherein the contrast is
enhanced by use of perfluorocarbon-filled
phospholipid microbubbles.
US Pat. Appl. 20060257490; November 16, 2006
Bioghurt Biogarde GmbH
Formulation based on phospholipids
The invention relates to a water-dispersable,
granulated formulation containing a fructane
constituent and a phospholipid constituent as a
physiologically active ingredient.
US Pat. Appl. 20060246126;November 2, 2006
Alza Corporation
Therapeutic liposome composition with
hydrogenated soybean phosphoatidylcholine and
method of preparation
R1H2O
R2H2O
+
O PO OCH2CH2N(CH3)3
Ophosphatidylcholine
Phosphatidylcholine is the main phospholipid of
crude lecithin. It is insoluble in acetone, soluble in
ethanol and dispersable in water under formation of
ordered structures. At neutal pH phosphatidylcholine
is a zwitterion which means it bears a positive and a
negative charge at the same time.
In pharmaceutics purified lecithin fractions with an
increased content in phosphatidylcholine are used
which are fractioned by solvent extraction and
column chromatography.
Analytical column
Iodine Value
US Pat. Appl. 20060233846; October 19, 2006
Phares Pharmaceutical Research N.V.
Microdispersion and method of producing same by
using hydrogenated phospholipids
The iodine value indicates how many grams of
halogen, calculated as iodine, are absorbed by 100g
of a sample material.
Information about a special phospholipid
It is a measure of the grade of unsaturation of the
material and is mainly used to analyse fats and oils.
The iodine value characterises each natural fat and
oil and is important for their identification. Therefore
it is part of each monograph and specification.
In the last issue we gave a short definition of the
term „lecithin“. Here we want to provide some
information about phosphatidylcholine.
It is also very useful for the characterisation of
partially or completely hydrogenated products.
_____________________________________________________________________________________________________________________
Phospholipid
Im Neuenheimer Feld 582
Phone +49 (0) 6221 - 5888360
Forschungszentrum / Research Center
D-69120 Heidelberg
Fax
+49 (0) 6221 - 6515665
Heidelberg
www.phospholipids.net
Newsletter Volume 2, Number 1
January 2007
Page 7
____________________________________________________________________________________________
There are used different variations of this analytical
method which give different results. Therefore the
method of analysis should always be mentioned
together with the result. The main variations are
according to Hanus, Sully, Wheeler, Kaufmann and
Wijs.
As natural phospholipids and lecithins contain,
depending on their origin, different fatty acids and
different amounts of fatty acids the iodine value is a
very useful method to determine their origin and also
the reproducibility of their production.
If a product contains different phospholipids
combined with triglycerides and other minor
components and different lots of this product show
very consistent iodine value the consistency of the
product is well proofed.
Contact
Phospholipid Research Center
Im Neuenheimer Feld 582
69120 Heidelberg
Germany
Phone: +49 (0)6221 / 5888360
Fax: +49 (0)6221 / 6515665
E-Mail: [email protected]
Web: www.phospholipids.net
_____________________________________________________________________________________________________________________
Phospholipid
Im Neuenheimer Feld 582
Phone +49 (0) 6221 - 5888360
Forschungszentrum / Research Center
D-69120 Heidelberg
Fax
+49 (0) 6221 - 6515665
Heidelberg
www.phospholipids.net