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The effect of thiamine-coating nanoparticles on their biodistribution and fate following oral administration

Lookup NU author(s): Dr Matthew Wilcox, Professor Jeffrey Pearson


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© 2018 Elsevier B.V. Thiamine-coated nanoparticles were prepared by two different preparative methods and evaluated to compare their mucus-penetrating properties and fate in vivo. The first method of preparation consisted of surface modification of freshly poly(anhydride) nanoparticles (NP) by simple incubation with thiamine (T-NPA). The second procedure focused on the preparation and characterization of a new polymeric conjugate between the poly(anhydride) backbone and thiamine prior the nanoparticle formation (T-NPB). The resulting nanoparticles displayed comparable sizes (about 200 nm) and slightly negative surface charges. For T-NPA, the amount of thiamine associated to the surface of the nanoparticles was 15 μg/mg. For in vivo studies, nanoparticles were labelled with either 99mTc or Lumogen® Red. T-NPA and T-NPB moved faster from the stomach to the small intestine than naked nanoparticles. Two hours post-administration, for T-NPA and T-NPB, >30% of the given dose was found in close contact with the intestinal mucosa, compared with a 13.5% for NP. Interestingly, both types of thiamine-coated nanoparticles showed a greater ability to cross the mucus layer and interact with the surface of the intestinal epithelium than NP, which remained adhered in the mucus layer. Four hours post-administration, around 35% of T-NPA and T-NPB were localized in the ileum of animals. Overall, both preparative processes yielded thiamine decorated carriers with similar physico-chemical and biodistribution properties, increasing the versatility of these nanocarriers as oral delivery systems for a number of biologically active compounds.

Publication metadata

Author(s): Inchaurraga L, Martinez-Lopez AL, Cattoz B, Griffiths PC, Wilcox M, Pearson JP, Quincoces G, Penuelas I, Martin-Arbella N, Irache JM

Publication type: Article

Publication status: Published

Journal: European Journal of Pharmaceutical Sciences

Year: 2019

Volume: 128

Pages: 81-90

Print publication date: 01/02/2019

Online publication date: 23/11/2018

Acceptance date: 22/11/2018

ISSN (print): 0928-0987

ISSN (electronic): 1879-0720

Publisher: Elsevier BV


DOI: 10.1016/j.ejps.2018.11.025


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