3rd International Symposium on Phospholipids in Pharmaceutical Research
16th – 17th September 2013 in Heidelberg, Germany
Peter van Hoogevest, PhD
Phospholipid Research Center, Heidelberg, Germany
This two day event was organized for the third time by the Phospholipid Research Center Heidelberg. The symposium was held at the University of Heidelberg (facilities provided by Prof. Gert Fricker) and visited by 170 scientists from academia, pharmaceutical industry, authorities etc. from all over the world. Sixty posters and sixteen lectures were presented. This year event started with lectures on the physico-chemical properties of phospholipids, followed by a systemic review of the administration route specific use of phospholipid. The second day of the event was devoted to the latest advances in application of phospholipids, followed by a session on the future use of phospholipids comprising oral presentations of selected posters, and a lecture on the appreciation of liposomes as nanotechnology. The symposium was concluded with an award ceremony of the three best posters.
Keywords: Phospholipids, Excipients, Drug Delivery, Nanotechnology
The symposium was opened on September 16, 2013 by Dr. Herbert Rebmann, chairman of the Phospholipid Research Center. The first scientific session on “Physico-Chemical Aspects of Phospholipids”, chaired by Dr. Frank Martin (San Francisco, USA) was opened by a key note lecture of Dr. Jürgen Zirkel (Ludwigshafen am Rhein, DE) on “A practical view on the use of phospholipids in pharmaceutical formulations”. He reviewed the chemical aspects and composition and analytical characterization of the various, nowadays available, natural and synthetic phospholipid excipients and their enormous versatility for use in pharmaceutical dosage forms for any administration route. Prof. Dr. Alfred Blume (Halle an der Saale, DE) illustrated in his plenary lecture on “Tuning the miscibility of lipids in multicomponent membranes” the influence of head group and fatty acid composition on the miscibility of the various phospholipid classes and the physico-chemical properties of the mixtures.
Prof. Dr. Christel Müller-Goymann (Braunschweig, DE) discussed in her lecture on “Functionalities of phospholipids in pharmaceutical preparations” the pharmaceutical technological use of phospholipids as emulsifiers and dispersants and the underlying physico-chemical mechanisms of these functionalities. Dr Andreas Wagner (Vienna, AT) informed on “Guiding liposomal therapeutics to clinical evaluation-points to consider in formulation and process development” and highlighted the quality aspects of phospholipids, process validation, analytics etc. in the GMP production of parenteral phospholipid based formulations. Finally, Dr. Toon de Kroon (Utrecht, NL) concluded the session on “Physico-Chemical Aspects of Phospholipids” with a seminar on the “intra- and inter-membrane dynamics of phospholipids in liposomal and biological membranes”.
The session on “Rational Selection of Phospholipids as Excipients” chaired by Prof. Dr. Gert Fricker (Heidelberg, DE) was opened by a key note lecture by PD Dr. P. van Hoogevest (Heidelberg, DE) on “Mother nature as guide for phospholipid excipient selection”. He pointed to the physiological action and importance of especially natural phospholipids, containing omega 3 and omega 6 fatty acids, which could be used, beside as technical excipients, to support the pharmacological action of the formulated drug substances or even be used for treatment of pathological conditions characterized by the absence of specific phospholipids. Examples were given on the physiological role of phospholipids and how these biological functionalities of phospholipids can be used to design optimal phospholipid based formulations. Dr. Mona Tawab (Eschborn, DE) gave a lecture on “Phospholipids as oral excipients”. She showed latest results on the determination of the affinity of various drug substances for mono- and diacylphospholipids. Especially, the monoacylphospholipids may have an enormous potential to be used as oral solubilizers for poorly water soluble drug substances. Prof. Alfred Fahr (Jena, DE) gave a lecture on “Phospholipids as parenteral solubilizers”. Phospholipids are nowadays used as parenteral solubilizers for Amphotericin B (AmBisome) and benzoporphyrin (Visudyne). The transfer properties of lipophilic drugs from liposomes to lipoproteins and phospholipid dependency of drug transfer kinetics were discussed. After the coffee break, Dr. Nathalie Wauthoz (Brussels, BE) reviewed “Phospholipids as pulmonary excipients and Dr. Majella Lane, “Opportunities for use of phospholipids in topical formulations”.
The second day of the symposium started with a session on “Latest advances in application of phospholipids”, chaired by Prof. Dr. Jörg Huwyler (Basle, CH). Dr Michal Heger (Amsterdam, NL) discussed the latest advances in “Photodynamic therapy of solid cancers with third-generation photosensitizers” and his research on zincphthalocyanine liposomes. Prof. Sandro Keller (Kaiserslautern, DE), discussed “Fusogenic peptides for phospholipids-based drug delivery” with a view to designing liposomes which are able to fuse with eventually target cells. The following two seminars were given on thermo-sensitive liposomes by PD Dr. Lars Lindner (Munich, DE) “Phosphatidyloligoglycerol-based temperature sensitive liposomes with improved PK profile” and Dr. Charles Sio (Eindhoven, NL) “Phospholipids in temperature sensitive liposomes for MR-HIFU (Magneticresonance guided high-intensity-focused-ultrasound) mediated drug delivery”. The seminars provided an interesting update on the use of specially designed thermo sensitive liposomes and the use of a highly sophisticated technology to locally induced hyperthermia to trigger the release of encapsulated drugs at the tumor site. The session was concluded by a seminar of Prof. Jan Kamps (Groningen, NL) on “Lipid based carriers for endothelial cell specific delivery of siRNA” with some highlights on his own research in this area.
The symposium was concluded by the session on “Future Use of Phospholipids” chaired by Prof. Dr. Christel Müller-Goymann (Braunschweig, DE). In a “Young Session” six 10 min presentations on preselected posters were given. The final seminar of Prof. Yechezkel Barenholz (Jerusalem, IL) on “Why today liposomes of all types of nano-particulate based formulations are the preferred choice of nano-drugs” made clear that the research and development experience obtained with liposomes and the presence of many liposome based nanotechnology products on the market, liposomes should be the first choice in selecting nano-carriers for drug targeting.
During the breaks of the symposium there was abundant opportunity to study Posters. The posters were categorized in the following areas: phospholipids, skin interaction, drug delivery, lipid analytics and pharmaceutical use. The following three posters were awarded and a prize of 500 € handed over by Prof. Dr. Christel Müller-Goymann (Braunschweig, DE):
- Thermosensitive liposomes encapsulating gemcitabine - an in-vivo feasibility study, Dr. Martin Hossann, Ludwig-Maximilians-University Munich, University Clinic Munich
- Matrix Liposomes – A solid liposomal formulation for oral administration, Silvia Pantze, Ruprecht-Karls University Heidelberg, Institute for Pharmacy and Molecular Biotechnology (IPMB)
- In vivo wholebody imaging using a liposomal quenched near-infrared dye, Dr. Ronny Rüger, Friedrich-Schiller-University Jena, Institute for Pharmacy
CONCLUSION AND THANKS
The symposium comprised excellent seminars and posters and was again an excellent place for networking. I would like to acknowledge the support given by the University of Heidelberg (Prof. Dr. Gert Fricker and his students), speakers, poster authors, chairmen, Scientific Advisory Board and Ms. Britta Merz. He pointed to the possibility to become member of the Phospholipid Research Center Heidelberg or to apply for a grant to support academic research on phospholipids (www. phospholipid-institute.com). The audience was thanked for their enthusiastic contributions and attention was drawn to the next International Symposium on Phospholipids in Pharmaceutical Research to be held in September 2015.