Supramolecular assemblies of cisplatin and polyelectrolytes: preparation, characterization and activity against cancer cells

D.B. Vieira, V. Kim, D.F.S. Petri, C.F.M. Menck, A.M. Carmona-Ribeiro
Universidade de São Paulo, BR

Keywords: nanoparticles, carboxymethylcellulose, chitosan, polyethyleneimine, human melanome and glioma cells


Nanoformulation of cisplatin (Cis) is important to circumvent its high toxicity against normal cells. In this work, Cis cationic nanoparticles were prepared by the self-assembly of drug and oppositely charged polyelectrolytes (carboxymethylcellulose, CMC; chitosan, CH; polyethyleneimine, PEI) over a range of concentrations ([Cis] = 25-250 nM; [CMC] = [CH ] = [PEI] = 0.1 mg/mL). The nanoparticle thereby obtained exhibited 70-200 nm mean diameter and 32 -48 mV of zeta-potentials. The effect of increasing the positive charge on particles was increasing cell death by apoptosis with charge density. In addition to the experiments with cancer cells other cells lines were also tested, which presented different sensibility to the drug. Against XPA and MRC5-SV cells, which are deficient and proficient cell lines in nucleotide-excision repair pathway, the formulations have differential cytotoxicity against the cells. Up to 250 nM Cis in the CMC/CH particles, the deficient cells were efficiently killed by apoptosis whereas the proficient cells were barely killed. The novel formulations have potential to deliver Cis also in vivo. Acknowledgments: Financial support from FAPESP and CNPq is gratefully acknowledged. DBV is the recipient of a Posdoctoral fellowship from FAPESP.