Preparation And Characterization Of Novel Chitosan Bearing Pendant Cyclodextrin Nanoparticles For Drug Delivery

(3-Cyclodextrin (P-CD) can form inclusion complexes with a variety of drugs, which can increase solubility, improve chemical and physical stability and/or enhance oral absorption of the drug. Chitosan (CS) is used as a bioadhesive polymer since and the CS has non-toxic, biodegradable, biocompatible. mucoadhesion.β-CD and CS have been widely used with drug delivery system. In this study, according to the advantages of both CD and CS derivative, we synthesized N-maleoyl chitosan bearing pendant cyclodextrin (CD-g-NMCS) and prepared CD-g-NMCS nanoparticles for drug delivery.In this study, the CD-g-NMCS polymer was synthesized by reacting maleic anhydride and chitosan bearing pendant cyclodextrin. which was prepared with CS and 6-OTs-β-CD, which was prepared with (3-CD and TsCl. The differentβ-CD substitute degrees (DSCD) of CD-g-CS could be obtained by adjusting mass ratio of 6-OTs-β-CD to CS, and confirmed by the 1HNMR, IR, XRD. Orthogonal experiments were used to optimize the reaction conditions. The different carboxyl substitute degrees (DSCOOH) of CD-g-NMCS could be obtained by adjusting mass ratio of maleic anhydride to chitosan bearing pendant cyclodextrin (CD-g-CS). CD-g-NMCS was confirmed by the 1HNMR. IR. XRD. The water-solubility, viscosity average molecular weight and cell toxicity of the CD-g-NMCS were examined.CD-g-CS (DSCD= 14.60%). CD-g-NMCS20 (DSCOOH= 21.2%) and CD-g-NMCS30 (DSCOOH= 30.5%) nanoparticles were obtained by ionic gelation method using sodium tripolyphosphate (TPP). which possessed spherical morphology, uniform size (190～280 nm), positive electrical charge (+20～+30 mV). Entrapment drug studies of the nanoparticles were conducted using ketoprofen (KTP) as a model drug. Various influencing factors in prepartion process were studied, and the drug release tests of the nanoparticles were carried out in vitro using PBS (pH= 4.0.6.8 and 7.4). The in vitro drug release study showed that the KTP-loaded CD-g-NMCS nanoparticles have prolonged release of drug. The in vitro release study indicated CD-g-NMCS nanoparticles had controlled-release effect. The nanoparticles were pH-sensitive. The degree of drug release from KTP-loaded CD-g-NMCS nanoparticles was depended on the DS of CD-g-NMCS. These results found that CD-g-NMCS nanoparticles was a new promising vehicle for controlled release drug.