Effects of pentapeptide conjugation on etoposide loaded polymeric micelles for the treatment of Cancer cells

Abstract

To getting the desirable therapeutic treatment for cancer, the efficacy and the reduction of toxicity of anticancer drugs are to be improvised. Although many of the drugs are in hydrophobic characteristics, the polymeric miceller delivery system would be the potential  way for the targeted delivery and the effective treatment of metastasis. The present study was documented that the hydrophobic drug, etoposide was encapsuled with the biodegradable block co polymer mPEG-PCL which further conjugated with the cell adhesion peptides YIGSR and EILDV peptides for targeting the laminin and fibronectin receptors respectively. The results revealed that the conjugated micelles having the affinity towards the tumour cells, thereby increase in cytotoxicity as well as anti -metastatic effects observed from the cell line studies using B16F10 melanoma cells. Interestingly, the study confirmed that the YIGSR peptide conjugated etoposide has more cytotoxic effects than the other Pentapeptide EIDLV conjugated etoposide. Also, to understand the predictable drug release in physiological conditions, the in-vitro release study was carried out with PBS at pH 7.4, observed the significant difference between the peptide conjugated micelles and the non-conjugated micelles. Further, lyophilization studies were carried out with different cryoprotectants / different ratios and the redispersibility index was calculated, observed that the single cryoprotectant was not retained the original particle size than the combinations. Overall, etoposide loaded-conjugated miceller formulations proved higher efficacy and reduced the toxicity in the treatment of cancer cells than the non-conjugated miceller formulations.