Chitosan-coated liposomes for intracellular oligonucleotides delivery: characteristics and cell uptake behavior.

Surface modification of liposomes with polymer to optimize drug delivery was well developed recently. The objective of the present work was to evaluate the feasibility of chitosan-coated liposomes (CSLP) as vehicles for anti-sense oligodeoxynucleotides (ASON). CSLP was obtained by adding chitosan dropwise to liposomes under magnetic stirring. The effect of chitosan content on size, zeta potential, and coating efficiency was investigated, which showed that chitosan increased the size and zeta potential of CSLP, and the coating efficiency increased with chitosan content increasing. Agarose gel electrophoresis was employed to evaluate the loading efficiency of CSLP for ASON, from which one could see ASON was completely combined to CSLP when the mass ratio of total lipids:ASON was more than 50:1. MTT assay showed that CSLP took on very low cytotoxicity, which is much lower than chitosan. At last, cell uptake behavior was investigated by a flow cytometer, which showed that CSLP enhanced significantly the COS7 cells uptake of ASON. All the results indicated that the CSLP could be a promising non-viral ASON vehicle.