Formulation and in Vitro Evaluation of Casein Nanoparticles as Carrier for Celecoxib
2020
Objective: The objective of this work was to formulate casein nanocarriers for the dissolution enhancement of poorly water soluble drug Celecoxib. Method: The celecoxib loaded casein nanocarriers viz., nanoparticles, reassembled casein micelles and nanocapsules were prepared using sodium caseinate as a carrier to enhance the solubility of celecoxib. The prepared formulations were characterized for particle size, polydispersity index, zeta potential, percentage entrapment efficiency, and surface morphology for the selection of best formulation. Fourier transform infrared spectroscopy, differential scanning calorimetry and X-ray powder diffraction study was used to for the confirmation of encapsulation of celecoxib. Further, in vitro drug dissolution, ex-vivo permeation studies on chicken ileum and stability studies were carried out. Result: The celecoxib loaded casein nanoparticles (batch A2) showed a particle size diameter 216.1 nm, polydispersity index 0.422 with percentage entrapment efficiency of 90.71% and zeta potential of -24.6 mV. Scanning electron microscopy of suspension confirmed globular shape of casein nanoparticles. The in vitro release data of optimized batch followed non Fickian diffusion mechanism. The ex vivo permeation studies on chicken ileum of celecoxib loaded casein nanoparticles showed permeation through mucous membrane as compared to pure celecoxib. The apparent permeability of best selected freeze dried celecoxib loaded casein nanoparticles (batch A2) was higher and gradually increased from 0.90 mg/cm2 after 10 min to a maximum of 1.95 mg/cm2 over the subsequent 90 min. A higher permeation was recorded at each time point than that of the pure celecoxib. Conclusion: The study explored the potential of casein as a carrier for solubility enhancement of poorly water soluble drugs.
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