Cocrystallization of gliclazide with improved physicochemical properties

Background Cocrystallization is one of the crystal engineering strategies used to alter the physicochemical properties of drugs that are poorly water-soluble. Gliclazide (GLZ), an antidiabetic drug, belongs to Biopharmaceutical Classification System class-II (low solubility and high permeability) an...

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Bibliographic Details
Published in:Future journal of pharmaceutical sciences 2021-06, Vol.7 (1), p.124-13, Article 124
Main Authors: Eesam, Shivarani, Bhandaru, Jaswanth S., Akkinepally, Raghuram Rao, Bobbala, Ravi Kumar
Format: Article
Language:English
Subjects:
Antidiabetics
Bioavailability
Cocrystallization
Crystal lattices
Drug delivery systems
Drugs
Gliclazide
In vitro dissolution
Medicine
Medicine & Public Health
Nanoparticles
Permeability
Pharmaceutical industry
Pharmaceutical sciences
Solubility
Spectrum analysis
Vibration
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Summary:Background Cocrystallization is one of the crystal engineering strategies used to alter the physicochemical properties of drugs that are poorly water-soluble. 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. 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 [3,5-dinitrosalicylic acid (DNS), 2,6-pyridine dicarboxylic acid (PDA), and L-proline (LPN)], and these were characterized using Differential Scanning Colorimetry (DSC), Powder X-ray diffraction (PXRD), Fourier Transform Infra-red spectroscopy (FTIR), and Raman spectral studies. Further, Scanning electron microscopy (SEM) analysis, accelerated stability, solubility, in vitro dissolution studies, and in vivo pharmacokinetic studies were performed in male Wistar rats. Results DSC and PXRD analysis confirmed the formation of the GLZ cocrystals. Hydrogen bonding between pure GLZ and its coformers was demonstrated based on FTIR and Raman analysis. SEM data showed morphological images for GLZ cocrystals differed from those of pure GLZ. In comparison with pure GLZ, these GLZ cocrystals have greatly improved solubility, in vitro dissolution, and in vivo profiles. 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). Conclusion Hence, cocrystallization of GLZ leads to improved physicochemical properties of poorly soluble drug gliclazide.
ISSN:2314-7253
2314-7245
2314-7253
DOI:10.1186/s43094-021-00261-z