Gold nanoparticles as an efficient drug delivery system for GLP-1 peptides.

In this work, the potential application of gold nanoparticles for GLP-1 analogues delivery was studied. For this purpose, the original sequence of the incretin GLP-1 was slightly modified in the C-terminal region by adding a cysteine residue to facilitate conjugation to the gold surface. The interaction between peptides and gold nanoparticles and also the colloid stability of the conjugates were studied by UV-vis spectrophotometry, TEM, IR and XPS spectroscopy. Moreover, the permeability of these conjugates was assayed using a Caco-2/goblet monolayer model. On the basis of the stability and permeability results, one of the conjugates was chosen to be administered intraperitoneally to normoglycemic rats. The intraperitoneal delivery of the GLP-1 analogue using gold nanoparticles led to decrease levels of blood glucose in the same way as native GLP-1, thereby demonstrating that the formulation of the analogue is stable in physiological conditions and maintains the activity of this incretin.

Hantzsch dihydropyridines: Privileged structures for the formation of well-defined gold nanostars.

Anisotropic and branched gold nanoparticles have great potential in optical, chemical and biomedical applications. However their syntheses involve multi-step protocols and the use of cytotoxic agents. Here, we report a novel one-step method for the preparation of gold nanostructures using only Hantzsch 1,4-dihydropyridines as mild reducing agents. The substituent pattern of the dihydropyridine nucleus was closely related to the ease of formation, morphology and stability of the nanoparticles. We observed nanostructures such as spheres, rods, triangles, pentagons, hexagons, flowers, stars and amorphous. We focused mainly on the synthesis and characterization of well-defined gold nanostars, which were produced quickly at room temperature (25°C) in high yield and homogeneity. These nanostars presented an average size of 68 nm with mostly four or six tips. Based on our findings, we propose that the growth of the nanostars occurs in the (111) lattice plane due to a preferential deposition of the gold atoms in the early stages of particle formation. Furthermore, the nanostars were easily modified with peptides remaining stable for more than six months in their colloidal state and showing a better stability than unmodified nanostars in different conditions. We report a new approach using dihydropyridines for the straightforward synthesis of gold nanostructures with controlled shape, feasible for use in future applications.