1: J Control Release. 2007 Jul 31;120(3):195-204. Epub 2007 May 22.

PEGylated PLGA-based nanoparticles targeting M cells for oral vaccination.

Garinot M, Fiévez V, Pourcelle V, Stoffelbach F, des Rieux A, Plapied L, Theate
I, Freichels H, Jérôme C, Marchand-Brynaert J, Schneider YJ, Préat V.

Université Catholique de Louvain, Unité de Pharmacie Galénique, Brussels,
Belgium.

To improve the efficiency of orally delivered vaccines, PEGylated PLGA-based
nanoparticles displaying RGD molecules at their surface were designed to target
human M cells. RGD grafting was performed by an original method called
"photografting" which covalently linked RGD peptides mainly on the PEG moiety of 
the PCL-PEG, included in the formulation. First, three non-targeted formulations 
with size and zeta potential adapted to M cell uptake and stable in
gastro-intestinal fluids, were developed. Their transport by an in vitro model of
the human Follicle associated epithelium (co-cultures) was largely increased as
compared to mono-cultures (Caco-2 cells). RGD-labelling of nanoparticles
significantly increased their transport by co-cultures, due to interactions
between the RGD ligand and the beta(1) intregrins detected at the apical surface 
of co-cultures. In vivo studies demonstrated that RGD-labelled nanoparticles
particularly concentrated in M cells. Finally, ovalbumin-loaded nanoparticles
were orally administrated to mice and induced an IgG response, attesting antigen 
ability to elicit an immune response after oral delivery.

PMID: 17586081 [PubMed - indexed for MEDLINE]

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