Synthesis and characterization of binary and ternary complexes of diclofenac with a methyl-β-CD and monoethanolamine and in vitro transdermal evaluation

Abstract

Here, we describe the chemical characterization of the inclusion complex between diclofenac (DCF) and methyl-β-cyclodextrin (M-β-CD) in the presence or absence of monoethanolamine (MEA). Several techniques were used to analyze the complex both in solution and in the solid state. Solubility of DCF was increased by the addition of M-β-CD. However, the DCF solubility increase was more significant by the addition of M-β-CD in the presence of MEA. In vitro permeation experiments through excised human skin revealed that DCF was enhanced by M-β-CD. Nevertheless, further improvement in the flux and the permeability coefficient of DCF was obtained by the ternary system DCF-M-ß-CD-MEA. The aim of our work was to develop a ternary inclusion complex of diclofenac with methyl-β-cyclodextrin and monoethanolamine. This complex may be a promising formulation for percutaneous administration of diclofenac.