ARTÍCULO

Optimization and evaluation of zein nanoparticles to improve the oral delivery of glibenclamide. In vivo study using C-elegans

Autores: Lucio Ollauri, David; Martínez Oharriz, María Cristina; Jaras, G.; Aranaz Oroz, Paula; González Navarro, Carlos Javier; Radulescu, A.; Irache Garreta, Juan Manuel
Título de la revista: EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
ISSN: 0939-6411
Volumen: 121
Páginas: 104 - 112
Fecha de publicación: 2017
Lugar: WOS
Resumen:
The aim of this work was to evaluate the capability of zein nanoparticles as oral carriers for glibenclamide (GB). Nanoparticles were prepared by a desolvation procedure in the presence of lysine as stabilizer. A central composite design was used to optimize this preparative process. Under the selected conditions, nanoparticles displayed a size of about 190 nm, a surface charge of -37 mV and a payload of 45 mu g GB/mg. Small-angle neutron scattering and X-ray diffraction techniques suggested an internal fractal-like structure, based on the repetition of spherical blocks of zein units (about 20 nm) grouped to form the nanoparticles. This structure, stabilized by lysine molecules located at the surface, would determine the release of GB (molecularly trapped into the nanoparticles) by a pure diffusion mechanism. Moreover, GB-loaded nanoparticles induced a significant hypolipidemic effect with a reduction of about 15% in the fat content of C. elegans worms. In addition, did not induce any significant modification in the lifespan of worms. In summary, the employment of zein nanoparticles as delivery systems of glibenclamide may be an interesting approach to develop new oral formulations of this antidiabetic drug.