Design and Development of Novel Anticancer Peptide Encapsulated Liposomes for Targeting of Solid Tumours In Vitro

Conventional cancer treatments possess limitations for solid tumours, such as lack of selectivity, thus nanomedicine is explored as an efficient tool in anticancer drug development. Therefore, this study aimed to design a novel anticancer peptide (ACP) and encapsulate it into a lipid-based nanoparticle for efficient delivery to tumours. ACP was designed using in silico methods and thereafter encapsulated into a liposomal formulation (P1CF1) using a thin-film hydration method. The shape, size, polydispersity index (PDI), and zeta potential (ZP) of the formulation were evaluated using cryo-transmission electron microscopy, and zetasizer, while the percentage drug encapsulation efficiency (%EE) and drug release were investigated using the ultra-filtration and the dialysis methods. The biocompatibility, cytotoxicity, and apoptosis activity of P1CF1 were evaluated using hemolysis, 3-[(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide] and annexin V-FITC/PI assays. P1CF1 was spherical, had a size of 193.46 ± 0.10 nm, a PDI of 0.342 ± 0.12, a ZP of -7.67 ± 0.04 mV, and an %EE of 91.23 ± 0,01%. Furthermore, P1CF1 was biocompatible at low concentrations, showed a controlled in vitro drug release, induced high cytotoxic (IC50 value of 2.967 µg/ml) and apoptosis effects on the cancer cells MCF-7 and was well tolerated by non-cancer HEK293 cells (IC50 value of 135.3 µg/ml). Overall, P1CF1 showed efficient encapsulation capacity, enhanced biocompatibility, and significant anticancer activity in tumour cells with minimum effect on healthy cells. These positive characteristics indicate potential in vivo applicability. Thus, future research can include in vivo evaluation of this novel formulation.