CDI cross-linked -cyclodextrin nanosponges of paliperidone: synthesis and physicochemical characterization

Paliperidone (PLP) is an antipsychotic drug indicated for treatment and management of schizophrenia. The current study demonstrates potential of PLP-loaded -cyclodextrin-based nanosponges (CDNS) for solubility enhancement and prolonged release of PLP. The inclusion complexes of PLP with carbonyldiimidazole (CDI) cross-linked nanosponges were synthesized. The drug-loaded CDNS were characterized for particle size, zeta potential, encapsulation efficiency, stability study, in vitro drug release studies. The interaction of PLP with CDNS was ascertained by FTIR, DSC and PXRD studies. The particle size and zeta potential values were sufficient to obtain stable formulations. Solubility was significantly increased and in vitro drug release studies revealed prolonged release of PLP from the CDNS for 6h. PXRD study revealed that the crystallinity of PLP was decreased due to complexation with the CDNS. Thus, cyclodextrin-based nanosponges represent a novel approach for solubility enhancement and improved dissolution of selected model drug PLP. [GRAPHICS] .