Liposomes as vehicled do increase water- solubility of new quinolones derivatives with promising anticancer activity

Aim The aim of this work was to investigate, to which extent four new quinolone-derivatives with promising anticancer activity may be incorporated within liposomes. For this purpose the liposomes technique has been investigated and the results are reported in this poster. Methods Each of the compounds was dissolved in methanol and mixed with methanolic solution of phosphatydilcholine. The solvent was evaporated at the roto evaporator. The film was resuspended with phosphate buffer (pH 7. 4) and the dispersion sonicated for reduce vesicle size. A modification of the analytical approach previously described by Saetern et al.1 was used to separate liposome-associated from free drug in order to quantify the amount of substances incorporated within the liposomes using the HPLC. Particle size was determinate using the PCS technique2 Result and discussion The incorporation studies have shown that all the compounds are solubilized using liposomes as carrier. A 200- to 500-fold increase in apparent solubility in aqueous medium was gained. Drug-to-lipid ratios in the range 2 to 5 µg/mg were obtained. Interestingly the four quinolone-derivatives have shown different association tendency with liposomes, probably due to the physico-chemical proprieties of the different group bonded in position 2 of the quiniolone ring