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The aim of this work was to encapsulate two drugs: 5-Fluorouracil (5-FU) with the hydrophobic properties and 5-Formyl-5,6,7,8-tetrahydropteroyl-L-glutamic acid calcium salt (leucovorin) with the hydrophilic properties into liposomes prepared by the modified reverse-phase evaporation method (mREV) from L-α-phosphatidylcholine dipalmitoyl (DPPC). The drugs are used in the anticancer multidrug therapy FLv (5-fluorouracil, leucovorin) and ELF (etoposide, leucovorin, 5-fluorouracil). We studied the competition for their encapsulation in liposomes 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. Liposomes are highly versatile structures for research, therapeutic and analytical applications. We concluded that the liposomes obtained by the mREV method may transport more than one drug simultaneously. [ABSTRACT FROM AUTHOR]

Abstract: The aim of this work was to encapsulate two drugs: 1-β-d-arabinofuranosylcytosine (Ara-C) with the amphiphilic properties and 5-fluorouracil (5-FU) with the hydrophobic properties into liposomes prepared by the modified reverse-phase evaporation method (mREV) from l-α-phosphatidylcholine dipalmitoyl (DPPC). Both drugs are used together in the anticancer multidrug therapy. We studied the competition for their encapsulation in liposomes 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. We concluded that the mREV method allows us to obtain liposomes which may transport more than one drug simultaneously. The NMR and UV studies of the drug competitive encapsulation and transport in liposomes formed from DPPC by the mREV method should be the basis for the analysis of the changes which may occur in vivo. [Copyright &y& Elsevier]

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) 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: H 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 of liposomes containing Ara-C did not significantly change while for the liposomes containing 5-FU it increased in comparison with T of the reference liposomes formed from DPPC. [ABSTRACT FROM AUTHOR]