Acetyl carnitine modified liposomes elevate cisplatin uptake in macrophage and cancer cells

This study aims to investigate the cellular uptake and cytotoxicity of surface-modified cisplatin (CisP) loaded liposomes by acetyl carnitine and polyethylene glycol (PEG) in macrophage and cancer cells. Blank and CisP loaded liposomal formulations modified/un-modified using cholesteryl acetyl carnitine (CAC) and PEG were prepared by ethanol injection and reverse micelle technique. In the following, they were characterized for size, size distribution, morphology, drug loading, in vitro drug release, and structural interaction studies. CisP analysis was performed by HPLC using complexation. Cytotoxicity and cellular uptake of the liposomes were then investigated in cancer cells of MCF7, HT29, A549, and macrophage cells of RAW264.7. Liposomal formulations showed spherical morphology with a particle size range of 99–138 nm, narrow size distribution, negative surface charge of −12.5 to −28.3, encapsulation efficiency of 84–88.2%, without certain interactions between components. CAC and CAC + PEG modified liposomes demonstrated higher cellular uptake and the corresponding CisP liposomes were also more cytotoxic in studied cell lines with some differences. Acetyl carnitine modification of CisP-liposomes can be considered an effective approach for increasing cellular uptake and cytotoxicity in studied cancer and macrophage cells.