Quality by design-based optimization of formulation parameters to develop quercetin nanosuspension for improving its biopharmaceutical properties

The present study describes the formulation, optimization and characterization of quercetin loaded nanosuspension. The formulation was prepared using liquid antisolvent precipitation technique. Optimization of formulation was done using Box Behnken design by varying the concentration of sodium lauryl sulfate and polyvinyl pyrrolidone that were used as solubilizers. The processing parameters varied in this study were mixing speed and solvent to antisolvent ratio. The optimized formulation showed particle size of 202.15 ± 3.56 nm, zeta potential -20.26 ± 1.32 mV and drug loading 95.22 ± 2.45%. The results of dissolution and permeability studies showed about 26 folds enhancement in dissolution rate and 3.35 folds enhancement in permeability of quercetin through nanosuspension as compared to its raw form.

Highlights

• Quercetin nanosuspension was formulated using antisolvent method.

• The formulation was optimized using box Behnken design.

• The particle size and zeta potential of nanosuspension were found to be 202.15 ± 3.56 nm, −20.26 ± 1.32 mV.

• The formulation showed 26 folds and 3.35 folds enhancement in dissolution and permeability of quercetin.

The results of cell viability studies performed on Caco2 cells indicated more than 90% cell viability upon using nanosuspension, indicating safety of developed formulation. Furthermore, the formulation was found stable at accelerated stability conditions indicating the marketing potential of the developed formulation. Overall results showed the appropriateness of the developed formulation in enhancing the biopharmaceutical properties of quercetin.

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Excipients used in the study besides others:

PVP K90, PVP K30, Tween 80, Pluronic F68, Pluronic F127, HPMC, HPC

Omar Awad Alsaidan, Prapti Pattanayak, Ankit Awasthi, Nabil K Alruwaili, Ameeduzzafar Zafar, Saud Almawash, Monica Gulati, Sachin Kumar Singh,
Quality by design-based optimization of formulation parameters to develop quercetin nanosuspension for improving its biopharmaceutical properties,
South African Journal of Botany, 2022, ISSN 0254-6299,
https://doi.org/10.1016/j.sajb.2022.04.030.