CDI cross-linked β-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 β-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 6 h. 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.

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We are thankful to Cadila Pharmaceuticals Ltd, India and Gangwal Chemicals Pvt. Ltd., Mumbai, India for gift sample of Paliperidone and β-CD, respectively.

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Correspondence to Atul P. Sherje.

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Sherje, A.P., Surve, A. & Shende, P. CDI cross-linked β-cyclodextrin nanosponges of paliperidone: synthesis and physicochemical characterization. J Mater Sci: Mater Med 30, 74 (2019).

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