The effect of m2 peptide targeted nanoliposomes containing crocin on induction of phenotypic change in tumor macrophages to M1 state

Abstract

AimsCrocin has immunomodulatory and anticancer effects. In this study, crocin was used to induce the M1 phenotype in mouse tumor macrophages. Main methodsA targeted liposomal formulation with m2 peptide was prepared and characterized to deliver crocin to the M2 macrophages present in the tumor environment. RT-qPCR and IHC were performed for in vitro and in vivo (in C26 colon carcinoma mouse model at a dose of 50 mg/kg) assessment of M1 induction, respectively. Key findingsIn vitro results indicated that liposome modified with m2 peptide was non-toxic to macrophages and had an improved uptake by macrophages compared to the non-targeted formulation and induced M1 phenotype through an IL6-independent pathway. M2 peptide- modified liposome showed considerable tumor accumulation and anti-tumor effects and significantly shifted the phenotype of tumor macrophages towards an anti-tumor M1 phenotype. SignificanceProbably the remarkable anti-tumor responses observed in this study with m2 peptide-targeted liposomal formulations containing crocin were due to the enhanced delivery of crocin to the tumor macrophage and the subsequent initiation of anti-tumor immune responses.