5-FLUOROURACIL - VARIOUS KINDS OF LOADED LIPOSOMES - ENCAPSULATION EFFICIENCY, STORAGE STABILITY AND FUSOGENIC PROPERTIES

This paper describes the optimization of 5-fluorouracil (5-FU) loaded liposome formulations. Four different preparation procedures were carr ied out, obtaining two types of multilamellar vesicles (MLVs), stable plurilamellar vesicles (SPLVs) and large unilamellar vesicles (LUVs). In this study various phospholipids were used to prepare liposomes. Th e lipid mixtures containing dipalmitoylphosphatidylserine seemed the b est for biological 5-FU delivery by presenting better encapsulation ef ficiency parameters, serum and storage stability, and fusogenic proper ties, which are an important prerequisite for in vivo liposome-cell in teraction. The presence of cholesterol in the liposome composition was an important factor thereby ensuring serum and storage stability of t he various vesicular systems. The most suitable liposome preparation w as the SPLVs, that showed both good drug loading and stability paramet ers, compared to LUVs which had the highest loading capacity but low s erum and storage stability.