Development and optimization of oral nanoemulsion of rutin for enhancing its dissolution rate, permeability, and oral bioavailability

Pharm Dev Technol. 2022 Jun;27(5):588-597. doi: 10.1080/10837450.2022.2090957. Epub 2022 Jun 22.

Abstract

Rutin-loaded nanoemulsion (NE-RU) formulation is the core research work in this report. Labrafil® M 1944 CS was used as the oil phase, Tween 80 as the surfactant, and Transcutol P as the co-surfactant in the preparation of nanoemulsion. By utilizing a three-level central composite design (CCD), the composition was optimized. The optimized formulation showed a droplet size of 98.53 ± 3.22 nm, zeta potential -46.70 ± 4.78 mV, and drug loading 92.34 ± 3.87%. The results of dissolution, permeability, and oral bioavailability showed about 25.55 folds, 1.98 folds, and 33.68 folds, respectively, in the case of NE-RU as compared to its naïve form. The response of fresh and aged NE was non-significantly different in terms of particle size, zeta potential, and drug loading, indicating that the formulation was stable. The successful development of NE-RU with an improved bioavailability profile suggested that this formulation might be used to examine the pharmacodynamics of oxidative stress-related metabolic disorders.

Keywords: Rutin; bioavailability; dissolution; nanoemulsion; permeability.

MeSH terms

  • Biological Availability
  • Emulsions
  • Nanoparticles*
  • Particle Size
  • Permeability
  • Rutin*
  • Solubility
  • Surface-Active Agents

Substances

  • Emulsions
  • Surface-Active Agents
  • Rutin