Abstract
This study aimed to evaluate the antitumor activity of PEGylated liposomal doxorubicin (Dox) functionalized with TAT peptide through PEG1000 while the surface of the liposome is covered by PEG2000 molecule. The size (nm) of liposomal formulations ranged from 90 to 140 nm, and all formulations had a negative zeta potential. The in vitro cellular uptake and cytotoxicity effects of formulations were investigated on C26 and B16F0 cell lines. Biodistribution and antitumor activity of formulations were investigated on BALB/c and C57BL/6 mice bearing C26 and B16F0 tumor models, respectively. In vitro and results on the C26 cell line indicated the higher efficacy of 100-ligand formulation, while in the case of B16F0 cell line 400-ligand formulation was the most efficient formulation. Since the TAT-peptide enters the cell through heparan sulfate proteoglycans, the difference in results may be due to the differences in expression levels and the intraspecies distribution between proteoglycans. Altogether our data indicate that surface-functionalization of liposome with TAT peptide via PEG1000 improves its antitumor efficacy and merit future considerations.
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The datasets used and/or analyzed during the current study are available from the corresponding author on reasonable request.
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This paper has been extracted from Farjad Zarazvand thesis. The authors would like to acknowledge the financial support of University of Tehran and Mashhad University of Medical Sciences.
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Zarazvand, F., Karimi, M., Moosavian, S.A. et al. Efficacy Comparison of TAT Peptide-Functionalized PEGylated Liposomal Doxorubicin in C26 and B16F0 Tumor Mice Models. Int J Pept Res Ther 27, 2099–2109 (2021). https://doi.org/10.1007/s10989-021-10238-4
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DOI: https://doi.org/10.1007/s10989-021-10238-4