In vitro and in vivo evaluation of YIGSR-modified liposomes co-loaded with doxorubicin and 5F

Targeted liposomes represent an excellent drug delivery system for enhancing therapeutic effects. In this study, a novel YIGSR-modified liposomal formulation co-encapsulating two antitumor drugs, doxorubicin (DOX) and ent-11α-hydroxy-15-oxo-kaur-16-en-19-oic-acid (5F), was developed to achieve good targeting capability and antitumor efficacy.The physicochemical properties of YIGSR-(DOX-5F)-LP were characterized and the liposomes exhibited a uniform particle size, high encapsulation efficiency and a sustained release profile. In vitro cytotoxicity assays indicated that YIGSR-(DOX-5F)-LP exerted the strongest cytotoxicity and highest levels of cellular apoptosis in DOX-sensitive MCF-7 cells. Its targeting ability was evaluated by in vitro cellular uptake assays in MCF-7 cells and in vivo biodistribution studies in tumor-bearing nude mice, respectively. The results showed that compared with non-targeted co-drug-loaded liposomes (DOX-5F-LP), YIGSR-(DOX-5F)-LP achieved higher cellular uptake in MCF-7 cells and exhibited greater accumulation in tumor tissues relative to other major organs. In conclusion, the YIGSR-(DOX-5F)-LP displayed prominent targeting activity toward MCF-7 cells both in vitro and in vivo, demonstrating a great potential for further preclinical investigation.