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

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Abstract

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 (X1) and poloxamer 188 concentration (X2) on the particle size (Y1) and entrapment efficiency (Y2; %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.

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Acknowledgements

This work is a Ph.D. research work of Mr. Haragouri Mishra registered under Centurion University of Technology and Management, Odisha, under the guidance of Dr. Amulyaratna Behra and Dr. Sidharth S. Kar.

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Authors and Affiliations

  1. School of Pharmacy and Life Sciences, Centurion University of Technology and Management, Bhubaneswar, Odisha, India

    Haragouri Mishra & Amulyaratna Behera

  2. Faculty of Pharmacy, C.V. Raman Global University, Bidyanagar, Mahura, Bhubaneswar, 752054, Odisha, India

    Sidhartha Sankar Kar

  3. Manipal College Pharmaceutical Sciences, Manipal, 576104, Karnataka, India

    Swagatika Dash

  4. School of Applied Sciences, Centurion University of Technology and Management, Bhubaneswar, Odisha, India

    Srikanta Moharana

  5. Nanotechnology & Catalysis Research Centre, University of Malaya, 50603, Kuala Lumpur, Malaysia

    Suresh Sagadevan

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Contributions

Concept — H.M., S.K.; design — H.M., S.D., S.K.; supervision — A.B.; resources —A.B., S.D.; materials — A.B.; data collection and/or processing — H.M., A.B.; analysis and/or interpretation — H.M., A.B., S.K., S.D.; literature search — H.M. A.B., S.D.; writing — H.M.; critical reviews — H.M., A.B., S.K., S.D, S.M and SS.

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Correspondence to Amulyaratna Behera, Sidhartha Sankar Kar or Suresh Sagadevan.

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Research Involving Humans and Animals Statement

Authors have followed all applicable international, national, and/or institutional guidelines for the care and use of animals. The animal studies were accomplished according to CPCSEA guidelines. The animal studies were approved by the Centurion University of Technology and Management, Odisha, India.

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We, all the author declares that there are no conflicts of interest among us. All the research facilities were provided by Centurion University of Technology and Management, Odisha. The animal experimentation was conducted as per the guidelines of CPCSEA (2024/PO/Re/S/18/CPCSEA) and approved by IAEC (CUTM/IAEC-03 dated 27/03/2023) of CUTM.

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Mishra, H., Behera, A., Kar, S.S. et al. Development and Optimization of Cefuroxime Axetil Nanosuspension for Improved Oral Bioavailability: In-Vitro and In-Vivo Investigations. BioNanoSci. 13, 2371–2384 (2023). https://doi.org/10.1007/s12668-023-01214-x

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