Evaluation of bioadhesive potential and intestinal transport of pegylated poly(anhydride) nanoparticles.

ABSTRACT

Nanoparticles based on the poly(methyl vinyl ether-co-maleic anhydride) were pegylated with different types of PEGs, namely, two hydroxyl-functionalized PEGs (PEG and mPEG) and two amino-PEGs (DAE-PEG and DAP-PEG). The resulted nanoparticles demonstrated reduction of the negative surface charge compared to the non-modified particles. Further, in vivo experiments showed that all types of pegylated particles possessed higher affinity to adhere to intestinal rather than to the stomach mucosa. Higher bioadhesive potential was observed in the case of PEG-NP and DAE-PEG-NP which was attributed to the flexibility and specific properties of the surface "brush" layer of these particles. The lower bioadhesive potential of mPEG-NP was due to the low presence of coating "brush" layer, whereas for DAP-PEG-NP to the fact that the double end coupled chains ("loop"-conformation) were not available for intensive interactions with the mucosa. The observations made by optic microscopy illustrated an intracellular transport of PEG-NP in vivo with preferable location in the apical area of enterocytes.