Modulation of the fate of zein nanoparticles by their coating with a Gantrez® AN-thiamine polymer conjugate
Inchaurraga L (1), Martínez-López AL (1), Abdulkarim M (2), Gumbleton M (2), Quincoces G (3), Peñuelas I (3), Martin-Arbella N (1), Irache JM (1).
(1) NANO-VAC Research Group, Department of Chemistry and Pharmaceutical Technology, University of Navarra, Spain.
(2) School of Pharmacy and Pharmaceutical Sciences, Cardiff University, Cardiff, UK.
(3) Radiopharmacy Unit, Department of Nuclear Medicine, Clinica Universidad de Navarra, University of Navarra, Spain.
The aim of this work was to evaluate the mucus-permeating properties of nanocarriers using zein nanoparticles (NPZ) coated with a Gantrez® AN-thiamine conjugate (GT).
NPZ were coated by incubation at different GT-to-zein ratios: 2.5% coating with GT (GT-NPZ1), 5% (GT-NPZ2) and 10% (GT-NPZ3). During the process, the GT conjugate formed a polymer layer around the surface of zein nanoparticles. For GT-NPZ2, the thickness of this corona was estimated between 15 and 20 nm.
These nanocarriers displayed a more negative zeta potential than uncoated NPZ. The diffusivity of nanoparticles was evaluated in pig intestinal mucus by multiple particle tracking analysis. GT-NPZ2 displayed a 28-fold higher diffusion coefficient within the mucus layer than NPZ particles.
These results align with in vivo biodistribution studies in which NPZ displayed a localisation restricted to the mucus layer, whereas GT-NPZ2 were capable of reaching the intestinal epithelium. The gastro-intestinal transit of mucoadhesive (NPZ) and mucus-permeating nanoparticles (GT-NPZ2) was also found to be different.
Thus, mucoadhesive nanoparticles displayed a significant accumulation in the stomach of animals, whereas mucus-penetrating nanoparticles appeared to exit the stomach more rapidly to access the small intestine of animals.
CITA DEL ARTÍCULO Int J Pharm X. 2019 Jan 25;1:100006. doi: 10.1016/j.ijpx.2019.100006. eCollection 2019 Dec