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Some of these techniques suffer from inherent problems, viz. Although effective in improving bioavailability, the utility of these techniques depends on the specific physicochemical nature of the molecule in question. Diverse techniques are available to improve the physicochemical properties of poorly soluble drugs such as nanoparticles, liposomes, microemulsions, nano-emulsions, carbon nanotubes, cyclodextrins, solid dispersions, nanoparticles, and self-micro emulsifying drug delivery systems, etc. Modification of solubility of poorly water-soluble drugs without compromising the stability is a particular challenge for the pharmaceutical industry. Such molecules would be ineffective in their bioactivity due to low solubility and permeability, limiting their therapeutic action. Developing these NCEs as suitable drugs into different dosage forms is becoming more challenging as many of them suffer from solubility issues. Hence, cocrystallization of GLZ leads to improved physicochemical properties of poorly soluble drug gliclazide.ĭrug discovery is a dynamic process resulting in a diverse set of new molecules as new chemical entities (NCE). Among the three, GLZ–DNS cocrystals outperformed the pure drug in terms of solubility (6.3 times), degradation (1.5 times), and relative bioavailability (1.8 times). In comparison with pure GLZ, these GLZ cocrystals have greatly improved solubility, in vitro dissolution, and in vivo profiles. SEM data showed morphological images for GLZ cocrystals differed from those of pure GLZ. Hydrogen bonding between pure GLZ and its coformers was demonstrated based on FTIR and Raman analysis. ResultsĭSC and PXRD analysis confirmed the formation of the GLZ cocrystals. Further, Scanning electron microscopy (SEM) analysis, accelerated stability, solubility, in vitro dissolution studies, and in vivo pharmacokinetic studies were performed in male Wistar rats. Therefore, to impart better solubility and bioavailability of GLZ, the study was carried out by preparing GLZ cocrystals using liquid-assisted grinding method with three coformers, and these were characterized using Differential Scanning Colorimetry (DSC), Powder X-ray diffraction (PXRD), Fourier Transform Infra-red spectroscopy (FTIR), and Raman spectral studies.
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Gliclazide (GLZ), an antidiabetic drug, belongs to Biopharmaceutical Classification System class-II (low solubility and high permeability) and has low bioavailability, resulting in poor therapeutic effects in patients. Cocrystallization is one of the crystal engineering strategies used to alter the physicochemical properties of drugs that are poorly water-soluble.