Bioadhesive properties and biodistribution of cyclodextrin-poly(anhydride) nanoparticles

This work describes the preparation, characterization and evaluation of the nanoparticles formed by the copolymer of methyl vinyl ether and maleic anhydride (Gantrez) AN) and cyclodextrins, including beta-cyclodextrin (CD) hydroxypropyl-beta-cyclodextrin (HPCD) and 6-monodeoxy-6-monoamino-beta-cyclodextrin (NHCD).

The cyclodextrin-poly(anhydride) nanoparticles were prepared by a solvent displacement method and characterized by measuring the size, zeta potential, morphology and composition.

For bioadhesion studies, nanoparticles were fluorescently labelled with rhodamine B isothiocianate (RBITC). For in vivo imaging biodistribution studies, (99m)Tc-labelled nanoparticles were used. Nanoparticles displayed a size of about 150nm and a cyclodextrin content which was found optimal under the following experimental conditions: cyclodextrin/poly(anhydride) ratio of 0.25 by weight, 30min of incubation time between the cyclodextrin and the polymer. Moreover, the oligosaccharide content was higher with CD than with NHCD and HPCD.

Overall, cyclodextrin-poly(anhydride) nanoparticles displayed homogeneous bioadhesive interactions within the gut. The intensity of these interactions was higher than for control nanoparticles.

The high bioadhesive capacity was observed for HPCD-NP and NHCD-NP which can be related with their rough morphology and, thus, a higher specific surface than for smooth nanoparticles (CD-NP). Finally, from in vivo studies, no evidence of translocation of distribution to other organs was observed when these nanoparticles were orally administered.R

CITATION  Eur J Pharm Sci. 2009 Jun 28;37(3-4):231-40.
doi: 10.1016/j.ejps.2009.02.010. Epub 2009 Feb 28