Influence of some physical properties of 5-fluorouracil on encapsulation efficiency in liposomes

Abstract

The aim of this study is to encapsulate two drugs: 5-fluorouracil (5-FU) with the hydrophobic properties and 1-β-D-arabinofuranosylcytosine (Ara-C) with the amphiphilic properties into liposomes prepared by the modified reverse-phase evaporation method (mREV) from L-α-phosphatidylcholine dipalmitoyl (DPPC). We studied the thermotropic phase behavior of liposome entrapped 5-FU and Ara-C. It is known that the stability of liposomes depends not only on the method of chemical gradient loading, the use of membrane stabilizer such as sterols, but also on the phase transition temperature (T c) of phospholipids, which undergoes an alteration after encapsulation of drugs to liposomes. The competition of these two drugs entrapped in liposomes was analyzed by the use of two spectroscopies: 1H NMR and UV on the basis of the analysis of the signals of each drug in the liposome—drug system. The percent of encapsulation in DPPC/Ara-C/5-FU liposome obtained by the use of UV spectroscopy amounted 93.84 and 96.05% for 5-FU and Ara-C, respectively. Phase transition temperature T c of liposomes containing Ara-C did not significantly change while for the liposomes containing 5-FU it increased in comparison with T c of the reference liposomes formed from DPPC.