RESUMO
The inclusion complex of picoplatin with γ-cyclodextrin (γ-CD) was prepared and characterised by different analytical methods, including NMR, FTIR, TGA, phase solubility as well as SEM. All of these approaches indicated that picoplatin was able to form an inclusion complex with γ-CD, and that the picoplatin/γ-CD inclusion compounds exhibited different spectroscopic features and properties from free picoplatin. The stoichiometry of the complex was 1:1; the pyridine group of picoplatin was deeply inserted into the cavity of γ-CD and the amine platinum group of picoplatin was near the narrower rim of γ-CD. The calculated apparent stability constant of the complex was 10,318M(-1). Moreover, the water solubility of picoplatin was significantly improved, according to phase-solubility studies. The complex maintained its anticancer activity, as shown by an in vitro cell-survival assay on A549 and MCF-7 cancer cell lines. All of these results showed that inclusion complexation may be a promising strategy to design a novel formulation of picoplatin as an anticancer therapy.
Assuntos
Antineoplásicos/química , Compostos Organoplatínicos/química , gama-Ciclodextrinas/química , Antineoplásicos/farmacologia , Varredura Diferencial de Calorimetria , Linhagem Celular Tumoral , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Concentração Inibidora 50 , Modelos Moleculares , Compostos Organoplatínicos/farmacologia , Solubilidade , Espectroscopia de Infravermelho com Transformada de Fourier , Termodinâmica , Difração de Raios X , gama-Ciclodextrinas/farmacologiaRESUMO
The reaction of cis-[Pt(NO(3))(2)(NH(3))(2)] and sodium glycolate yielded the title compound, [Pt(C(2)H(2)O(3))(NH(3))(2)]. The Pt(II) atom, coordinated by two N atoms of ammine and two O atoms of the carboxyl-ate and oxido groups of the glycolate ligand, is in a square-planar environment. In the crystal structure, mol-ecules are connected by inter-molecular N-Hâ¯O hydrogen bonds, forming a three-dimensional network.
