Oral Bioavailability Improvement of Tailored Rosuvastatin Loaded Niosomal Nanocarriers to Manage Ischemic Heart Disease: Optimization, Ex Vivo and In Vivo Studies

Abstract

Rosuvastatin is an efficient antihyperlipidemic agent; however, being a BCS class II molecule, it shows poor oral bioavailability of < 20%. The present study focused on the improvement of oral bioavailability of rosuvastatin using tailored niosomes. The niosomes were prepared by film hydration method and sonication using cholesterol and Span 40. The Box-Behnken design (BBD) was applied to optimize the size (98 nm) and the entrapment efficacy (77%) of the niosomes by selecting cholesterol at 122 mg, Span 40 at 0.52%, and hydration time at 29.88 min. The transmission electron microscopy image showed spherical shape niosomes with smooth surface without aggregation. The ex vivo intestinal permeability studies showed significant improvement in the rosuvastatin permeation (95.5% after 2 h) using niosomes in comparison to the rosuvastatin suspension (40.1% after 2 h). The in vivo pharmacokinetic parameters in the rat model confirmed the improvement in the oral bioavailability with optimized rosuvastatin loaded niosomes (relative bioavailability = 2.01) in comparison to the rosuvastatin suspension, due to high surface area of niosomes and its lymphatic uptake via transcellular route. In conclusion, the optimized rosuvastatin loaded niosomes offers a promising approach to improve the oral bioavailability of rosuvastatin.

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Data Availability

The raw data are available on request to the corresponding author.

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Liu, Q., Xu, J., Liao, K. et al. Oral Bioavailability Improvement of Tailored Rosuvastatin Loaded Niosomal Nanocarriers to Manage Ischemic Heart Disease: Optimization, Ex Vivo and In Vivo Studies. AAPS PharmSciTech 22, 58 (2021). https://doi.org/10.1208/s12249-021-01934-x

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KEY WORDS

  • rosuvastatin
  • niosomes
  • Box-Behnken design
  • pharmacokinetic studies