OPTIMIZATION AND IN VITRO EVALUATION OF 5-FLUOROURACIL –
LOADED LONG – CIRCULATING LIPOSOMES
MARCELA ACHIM1, IOAN TOMUȚĂ1*, DANA MUNTEAN1, ALINA PORFIRE1, LUCIA RUXANDRA TEFAS1, LAURA PATRAS2,3, EMILIA LICARETE2,3, MARIUS COSTEL ALUPEI2,3, LAURIAN VLASE1, MANUELA BANCIU2,3
1Department of Pharmaceutical Technology and Biopharmacy, Faculty of Pharmacy, “Iuliu Hațieganu” University of
Medicine and Pharmacy, 41 Victor Babeș Street, 400012 Cluj-Napoca, Romania
2Department of Molecular Biology and Biotechnology, Faculty of Biology and Geology, “Babeș-Bolyai” University, 400006,
Cluj-Napoca, Romania
3Molecular Biology Centre, Institute for Interdisciplinary Research in Bio-Nano-Sciences, “Babeș-Bolyai” University,
400271, Cluj-Napoca, Romania
*corresponding author: tomutaioan@umfcluj.ro
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Abstract:
5-Fluorouracil (5-FU) is an anticancer drug widely used in the treatment of colorectal cancers. In this work, long-circulating
liposomes (LCL) were proposed as carriers able to improve the therapy with 5-FU. The objective was to optimize the
formulation of 5-FU-loaded long circulating liposomes (LCL-5-FU) using the method of experimental design and to evaluate
the in vitro drug release and cytotoxicity on C26 murine colon carcinoma cells cultivated in monoculture as well as in coculture
with murine peritoneal macrophages. The influence of phospholipids concentration and phospholipids to cholesterol
molar ratio was studied on 5-FU liposomal concentration, entrapment efficiency and liposomes’ size. The optimized
formulation (LCL-5-FU-OPT) had liposomal 5-FU concentration of 331.4 μg/mL, entrapment efficiency of 3.18 % and
liposomes’ size of 200 nm. The in vitro release test has shown a diffusion of 5-FU of 90% in 3 hours. The cytotoxicity data
indicated that LCL-5-FU-OPT exerted strong and similar inhibitory effects on the proliferation of C26 tumour cells under both
culture conditions as those exerted by free 5-FU administration. In conclusion, the liposomal 5-FU formulation optimized
within our studies might offer promise for future anti-cancer therapies based on passive tumour targeting by using LCL.






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