DEVELOPMENT OF OLMESARTAN MEDOXOMIL-LOADED CHITOSAN MICROPARTICLES: A POTENTIAL STRATEGY TO IMPROVE PHYSICOCHEMICAL AND MICROMERITIC PROPERTIES
Objective: The objective of the present research was to improve physicochemical and micromeritic properties of Olmesartan Medoxomil (OLM), BCS class II antihypertensive drug by loading in Chitosan (CH) microparticles.
Methods: The 32 full factorial design was assigned for microparticles prepared by single emulsion technique method using CH, a natural polymer and Glutaraldehyde (GA) as cross linking agent. Developed microparticles were characterized for Micromeritic properties, morphology by Scanning Electron Microscopy (SEM), drug entrapment efficiency, in vitro drug release, and interaction studies Fourier transfer infrared spectroscopy (FTIR) & Differential Scanning Calorimetry (DSC), drug crystallinity study by X-ray diffractometry (XRD) & DSC.
Results: Maximum entrapment efficiency was found 61.76% for maximal CH and lower GA concentration. Saturation solubility of microparticles was increased by 13.74 times to that of pure OLM. FTIR showed compatibility between drug and polymer. XRD, DSC and SEM studies confirmed reduction in crystallinity of drug. It led to increase in dissolution profile of the drug and showed 92.61% of drug release in 120 min. These microparticle preparations also helped in improving micromeritic properties like bulk density, tapped density, the angle of repose, Hausnerâ€™s ratio and Carrâ€™s index.
Conclusion: The results obtained in the present work demonstrate the potential use of CH to modulate physicochemical and micromeritic properties of OLM especially obtaining significant improvement in dissolution rate.
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