Development and Optimization of Cefuroxime Axetil Nanosuspension for Improved Oral Bioavailability: In-Vitro and In-Vivo Investigations

• Published in: BioNanoScience Vol. 13; no. 4; pp. 2371 - 2384
• Main Authors: Mishra, Haragouri, Behera, Amulyaratna, Kar, Sidhartha Sankar, Dash, Swagatika, Moharana, Srikanta, Sagadevan, Suresh
• Format: Journal Article
• Language: English
• Published: New York Springer US 01.12.2023; Springer Nature B.V
• Subjects: Amorphization; Bioavailability; Biological and Medical Physics; Biomaterials; Biophysics; Cefuroxime; Chemical precipitation; Circuits and Systems; Differential scanning calorimetry; Engineering; Entrapment; Factorial design; Fourier transforms; Infrared spectrophotometers; Infrared spectroscopy; Nanoparticles; Nanotechnology; Particle size; Poloxamers; Scanning electron microscopy; Spectrophotometry; Stirring; X ray powder diffraction; X-ray diffraction; Zeta potential; Nanoparticles; Ultrasonication; Anti-solvent precipitation; Factorial design; Amorphization; Solubility
• ISSN: 2191-1630; 2191-1649
• DOI: 10.1007/s12668-023-01214-x

Cefuroxime axetil is a significantly used in drug formulation. Therefore, this study aimed to prepare a nanosuspension of cefuroxime axetil, a poorly water-soluble drug, using an antisolvent precipitation method, followed by ultrasonication. A 32 factorial design was used, and the effects of stirring speed ( X 1 ) and poloxamer 188 concentration (X 2 ) on the particle size (Y 1 ) and entrapment efficiency ( Y 2 ; %EE) of the prepared nanosuspension were investigated. The nanoparticles were characterized using scanning electron microscopy (SEM), Fourier transform infrared spectrophotometry (FTIR), powder X-ray diffraction (XRD), differential scanning calorimetry (DSC), and zeta potential analysis. The bioavailability of the formulation was assessed in rats. The results indicated that increasing the stirring speed and reducing the poloxamer concentration decreased the size of the nanoparticles. The optimized formulation showed particle size and zeta potential of 170 nm and − 31.3 mV, respectively. FTIR analysis revealed no incompatibilities between the formulation components. XRD and DSC analyses confirmed the amorphization of cefuroxime axetil in the nanosuspension. The developed nanoformulation showed 10.98-fold improvement in the oral bioavailability of cefuroxime axetil. The anti-solvent precipitation process successfully produced a stable amorphous nanosuspension with a notably reduced particle size and improved bioavailability by evaluating and optimizing the critical process and formulation parameters.