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Characterization of physical interaction between Casiopeina III-ia and chitosan. Toward a Cas III-ia drug delivery system

Miranda-Calderón, J.E., Medina-Torres, L., Tinoco-Mendez, M., Moreno-Esparza, R., Ruiz-Ramirez, L., Gracia-Mora, J., Gracia-Mora, I., Bernad-Bernad, M.J.
Carbohydrate research 2011 v.346 no.1 pp. 121-126
acetic acid, anticarcinogenic activity, antineoplastic agents, chemical interactions, chitosan, copper, drug delivery systems, electrostatic interactions, nanoparticles, organometallic compounds, pH, viscosity
Casiopeínas® are a new generation of anticancer drugs that have shown great in vitro and in vivo antineoplastic activities. Information about interaction drug-excipient, for developing a based-nanoparticle drug delivery system, has not been investigated yet. In order to elucidate if chitosan (CS) modifies the copper complex due to its interaction with Cu²⁺ ion, different studies in aqueous media between CS and Casiopeina III-ia (Cas III-ia) were carried out. CS–Cas III-ia mixtures were characterized by viscosity curves, UV–vis, EPR, and in vivo activity against HeLa cell line. Rheological behavior showed a decrease of viscosity when the drug was present due to diminished electrostatic interactions of charged amine group. UV–vis results illustrate that Cas III-ia is not stable at low pH as a result of interaction with acetic acid. However, when chitosan is present at the acidic solution Cas III-ia is stable. These results are supported by EPR studies. Finally, activity of the drug against HeLa cell line was not modified. Therefore, the present work presents evidence that there is no breaking of copper complex due to interaction between CS and Cas III-ia in acidic media. In addition, Cas III-ia maintains both its stability and effectiveness against cancer cell line.