Abstract
Gold(I) phosphane compounds have recently attracted a renewed interest as potential new protagonists in cancer therapy. A class of phosphane gold(I) complexes containing azolate ligands has been successfully tested against several cancer cell lines and, in particular, against basal-like breast (BLB) cancer, a form characterized by strongly severe diagnosis and short life lapse after classic chemotherapy. Even though the anticancer activity of gold(I) phosphane compounds is thoroughly ascertained, no study has been devoted to the possibility of their delivery in nanovectors. Herein, nonlamellar lyotropic liquid crystalline lipid nanosystems, a promising class of smart materials, have been used to encapsulate gold(I) azolate/phosphane complexes. In particular, ((triphenylphosphine)-gold(I)-(4,5-dichloroimidazolyl-1H-1yl)) (C-I) and ((triphenylphosphine)-gold(I)-(4,5-dicyanoimidazolyl-1H-1yl)) (C-II) have been encapsulated in three different lipid matrices: monoolein (GMO), phytantriol (PHYT) and dioleoyl-phosphatidylethanolamine (DOPE). An integrated experimental approach involving X-ray diffraction and UV resonant Raman (UVRR) spectroscopy, based on synchrotron light and attenuated total reflectance Fourier transform infrared (ATR-FTIR) spectroscopy, has been employed to establish the effects of drug encapsulation on the structure and phase behavior of the host mesophases. The results indicate that gold(I) complexes C-I and C-II are successfully encapsulated in the three lipid matrices as evidenced by the drug-induced phase transitions or by the changes in the mesophase lattice parameters observed in X-ray diffraction experiments and by the spectral changes occurring in UV resonant Raman spectra upon loading the lipid matrices with C-I and C-II.
Highlights
A continuous research effort is in progress for the production of efficient drug nanocarriers for anticancer therapy having formulations with a higher degree of specificity and reduced adverse effects
The structural investigation was carried out by SAXS, UV-Raman and ATR-FTIR measurements to study the influence of the gold(I) compounds on the three different lipid matrices glyceryl monooleate or monoolein (GMO), PHYT and DOPE, and to explore the specific interactions of the gold(I) compounds with the carriers
The aim of SAXS investigation was to assess if gold compounds arrange in the lipid matrices, each one characterized by a different phase symmetry, by studying the structural changes induced by drug loading
Summary
A continuous research effort is in progress for the production of efficient drug nanocarriers for anticancer therapy having formulations with a higher degree of specificity and reduced adverse effects. Cubosome and hexosome systems, in which the lipid bilayers are arranged in periodic two and three dimensional lattice structures, represent attractive smart delivery matrices for drugs and/or diagnostic agents with different water affinity [5,6,7,8,9,10,11,12,13]. The stiffness of these phases can lead to a slower diffusion of the solubilized cargo and to a long-term release Within this frame, we are currently developing bio-systems based on hexagonal and cubic phases dispersed in a continuous aqueous medium, which could find a potential application as anticancer drug delivery vectors. A multitask characterization involving small-angle X-ray diffraction (SAXS), UV resonant Raman (UVRR) and attenuated total reflectance Fourier transform infrared (ATR-FTIR) spectroscopy was employed to establish the effects of gold compounds encapsulation on the structure and phase behavior of the mesophases. The optimized (no symmetry constraints imposed) C-I and C-II molecules were used for Raman and IR spectrum calculation
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