Paliperidone-Benzamide Cocrystals: Preparation, Characterization, In Vitro/In Vivo Evaluation

The current investigation contributes in the development of novel Paliperidone (PPD) co-crystals (CCs) using benzamide (BZ) as a conformer. The CCs were synthesized using solvent evaporation technique. The enhancement in solubility was studied by saturation solubility studies. Structural characterization of CCs was performed by Fourier Transform Infra-Red Spectroscopy (FTIR), powder X-ray diffraction (PXRD), Differential Scanning Calorimetry (DSC), Scanning Electron Microscopy (SEM) and Proton Nuclear Magnetic Resonance (1H- FT NMR) to verify CC formation. CCs exhibited higher aqueous solubility of 2.067±0.004mg/ml when compared to pure drug 0.473±0.012mg/ml. This designated aqueous solubility enhancement of CCs by 4.36 folds. In vitro dissolution data of the CCs exhibited a drug release of 96.5±1.63% in 60min, while pure drug showed a poor release of 37.8±1.76% in the same time period In vivo CCs formed between PPD and BZ present a novel approach in overcoming the hurdles in the solubility of PPD that exhibits poor aqueous solubility.