Besides its use in gouty arthritis, colchicine has been found to be useful for anticancer treatment. However, the severe toxicity and low therapeutic index of colchicine limit its therapeutic use. It was hypothesized that toxicity of colchicine can be reduced if it is encapsulated in liposomes. The objective of this study was to determine and compare in vitro cellular uptake and cytotoxicity of colchicine with that of liposome encapsulated colchicine. Colchicine was encapsulated in negatively charged unilamellar liposomes (LUVs). Two cell lines, human macrophages (U-937) and murine myeloma (B-type, P3X63.Ag8.653) cells were used for these investigations. Cells were incubated with colchicine or liposomal colchicine and cellular uptake was determined by means of radioactive labeled colchicine. Cytotoxicity was determined by MTT (3-[4,5-dimethylthiazol- 2-yl]-2,5-diphenyltetrazolium bromide) assay. Human macrophages as well as murine myeloma cells showed greater uptake of liposomal colchicine than plain colchicine. However, cytotoxicity of liposomal colchicine to human macrophages was less compared to that of plain colchicine. On the other hand, in the case of murine myeloma cells, cellular uptake as well as cytotoxicity was greater with liposomal colchicine than that with plain colchicine. These results indicate that liposomal encapsulation of colchicine could avoid or reduce its toxicity and improve therapeutic efficacy.
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