Preparation and characterization of -cyclodextrin grafted -maleoyl chitosan nanoparticles for drug delivery.

-cyclodextrin (CD) grafted N-maleoyl chitosan (CDNMCS) with two different degrees of substitution (DS) of -maleoyl (DS = 21.2% and 30.5%) were synthesized from maleic anhydride and chitosan bearing pendant cyclodextrin (CDCS). CDNMCS based nanoparticles were prepared via an ionic gelation method together with chitosan and CDCS nanoparticles. The size and zeta potential of prepared CDNMCS nanoparticles were 179.2274.0 nm and 36.242.4 mV, respectively. stability test indicated that CDNMCS nanoparticles were more stable in phosphate-buffered saline compared with chitosan nanoparticles. Moreover, a poorly water-soluble drug, ketoprofen (KTP), was selected as a model drug to study the obtained nanoparticle's potentials as drug delivery carriers. The drug loading efficiency of CDNMCS20 nanoparticles were 14.8% for KTP. MTT assay showed that KTP loaded CDNMCS nanoparticles were safe drug carriers. Notably, drug release studies showed that KTP was released in a sustained-release manner for the nanoparticles. The pharmacokinetic of drug loaded CDNMCS20 nanoparticles were evaluated in rats after intravenous administration. The results of studies revealed that, compared with free KTP, KTP loaded CDNMCS20 nanoparticles exhibited a significant increase in AUC and mean residence time by 6.6-fold and 2.9-fold, respectively. Therefore, CDNMCS nanoparticles could be used as a novel promising nanoparticle-based drug delivery system for sustained release of poorly water-soluble drugs. The carboxylic acid groups of the CDNMCS molecule provide convenient sites for further structural modifications including introduction of tissue- or disease- specific targeting groups.