S U P R A M O L E C U L A R    C H E M I S T R Y
 
Liposomes as vectors for drug delivery
 
Since a few years we have a collaboration with the Italian pharmaceutical company Sigma-Tau in Pomezia (Roma). This company has developed hundreds of carnitine derivatives, including some these compounds function well as surfactants. One of the aim of the company is the application of such carnitine surfactants as basis for the formation of vesicles that can be used for drug delivery systems. One such system is PUCE, palmitoyl undecyl carnitine ester, that forms spontaneously cationic vesicles in water. 
In addition, the company is also interested in the commercialization of a camptothecin derivative (CPT), a powerful drug against certain types of tumor. 
Over the last years - 2000 and 2001, first Cornelia Heiz (graduated in 1999), then Dr. Jörg Heerklotz and Dr. Elisa Peroni  have been working in our lab in Zürich in a project aimed at preparing CPT-containing vesicles from PUCE. 
Mostly the injection method has been used for the preparation of PUCE vesicles, and conditions have been found, under which very small (30-60 nm radius) vesicles that contained a therapeutically sufficient amount of CPT could be prepared. Biological studies with animals have given very promising  results. This vesicle preparation obtained with the injection method has been compared with one prepared from a thin lipid film deposited on glass by a classic vesicle formation method. In addition, comparison is in progress between PUCE and POPC vesicles in terms of transport of CPT and the biological activity. 
Gene transfer experiments have been also carried out, utilizing a plasmid containing the gene of a fluorescent protein as label for the transfection efficiency. To this aim, PUCE vesicles bearing a positive charge have proved to be efficient vectors for DNA; these vesicles are being compared in terms of transport efficiency with POPC liposomes containing variable amounts of the classic cationic surfactant DDAB (dioctadecyldimethylammonium bromide). Biological activity with PUCE liposomes again appears to be very promising. 
One work that was initiated by Cornelia Heiz with liposomes as drug delivery systems concerns liposomes as an aerosol preparation. This work was carried out in collaboration with the “Kantonsspital” in Bern, in a project aimed at finding alternative routes to methadon for drug addicts, thus eliminating the use of syringes. 
At the end of 2001 both Jörg Heerklotz and Elisa Peroni left the group, and their work is now continued and developed by Simone Bufali and Pasquale Stano. They have also the function of being responsible of the two dynamic light scattering instruments we have in the group, and the corresponding data elaboration.