[Preparation of 5-fluorouracil encapsulated in amphiphilic polysaccharide nano-micelles and its killing effect on hepatocarcinoma cell line HepG2].
OBJECTIVE
Biodegradable colloidal nano-micelles is a novel targeting drug delivery and controlled release system, which could prolong the biological half-life and lighten the toxicity of chemotherapeutant, meanwhile, present fine biocompatibility. This study was to prepare the biodegradable 5-fluorouracil (5-FU)/DEX-g-PLA nano-micelles, and investigate their killing effect on hepatocarcinoma cell line HepG2 in vitro and in vivo.


METHODS
5-FU/DEX-g-PLA nano-micelles were prepared by 'self-assembly'. Its morphology was observed by transmission electron microscopy. The encapsulating efficiency of 5-FU was determined by ultraviolet spectrophotometry. The in vivo releasing of 5-FU from nano-micelles was investigated by high-performance liquid chromatography (HPLC). The inhibitory effect of 5-FU/DEX-g-PLA on HepG2 cells in vitro was measured by MTT assay.


RESULTS
5-FU/DEX-g-PLA nano-micelles were round or elliptical; the diameter was about 50 nm. The encapsulating efficiency was about 9.3%. The concentration of 5-FU released from 5-FU/DEX-g-PLA nano-micelles was sustained for longer time than that of the naked drug. The in vitro inhibition rate of cell growth was similar in 5-FU/DEX-g-PLA group and naked 5-FU group (58.8% vs. 58.0%, P>0.05); the in vivo inhibition rate of tumor growth was significantly higher in 5-FU/DEX-g-PLA group than in naked 5-FU group (73.1% vs. 57.5%, P<0.05).


CONCLUSIONS
5-FU/DEX-g-PLA nano-micelles can effectively inhibit the growth of HepG2 cells.
Zhou
Jia-Jia
JJ
Department of Hepatobiliary Surgery, The Second Affiliated Hospital, Sun Yat-sen University, Guangzhou, Guangdong, 510120, P. R. China.
Chen
Ru-Fu
RF
Tang
Qi-Bin
QB
Zhou
Quan-Bo
QB
Lu
Hong-Wei
HW
Wang
Jie
J
D000818:Animals; D000964:Antimetabolites, Antineoplastic / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology*; D006528:Carcinoma, Hepatocellular / Q000378:metabolism / Q000473:pathology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects*; D003911:Dextrans; D005260:Female; D005472:Fluorouracil / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology*; D007773:Lactates; D008297:Male; D051379:Mice; D008823:Micelles; D053758:Nanoparticles; D009368:Neoplasm Transplantation; D011092:Polyethylene Glycols; D011897:Random Allocation; D047368:Tumor Burden / Q000187:drug effects
D000964:Antimetabolites, Antineoplastic; D003911:Dextrans; D007773:Lactates; D008823:Micelles; C088513:poly(lactic acid-ethylene glycol); D011092:Polyethylene Glycols; D005472:Fluorouracil