Scientific publications

Modulation of the fate of zein nanoparticles by their coating with a Gantrez® AN-thiamine polymer conjugate

Jan 25, 2019 | Magazine: International Journal of Pharmaceutics: X

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).

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.

CITATION  Int J Pharm X. 2019 Jan 25;1:100006. doi: 10.1016/j.ijpx.2019.100006. eCollection 2019 Dec