Gemcitabine was loaded in albumin nanoparticles then coated with chitosan. The diameter of GEM-ANPs/CS was 200 ± 4 nm. Gemcitabine was loaded in GEM-ANPs/CS with an efficacy of 75%. The IC50 of GEM-ANPs/CS was found to be 12.98 and 6.08 μg/ml after incubation for 48 and 72 h with MCF-7 cells, respectively. Treatment of MCF-7 cells with IC50 of GEM-ANPS, and GEM-ANPS/CS resulted in membrane damage which led to elevated LDH activity of 4 and 3.4, and increasing GSH level of 4.6 and 9.3, respectively, when compared with untreated cells. DNA fragmentation and up-regulated of caspase-3 and p53 had illustrated the apoptotic effect of MCF-7 treated with GEM-ANPS/CS. The tumour suppressor RRM1 gene expression was down-regulated in MCF-7 cells treated with GEM-ANPS/CS. The modified ANPs coated with chitosan may be used as a promising nanomatrix for gemcitabine delivery and targeting to improve its therapeutic index against MCF-7 cells.
Keywords: Albumin nanoparticles; MCF-7; apoptosis; chitosan; gemcitabine.