1Department of Pharmaceutics, K.L. College of Pharmacy, Koneru Lakshmaiah Education Foundation, Vaddeswaram, INDIA
2Department of Pharmaceutical Engineering, B V Raju Institute of Technology, Medak, INDIA
3Department of Chemical Engineering, Chaitanya Bharathi Institute of Technology (CBIT), Hyderabad, INDIA
Corresponding author.
Author Notes
Copyright and License information
ABSTRACT
Background
Rosuvastatin (ROS) is an anti-hyperlipidaemic drug which reduces cholesterol levels, having poor solubility and low bioavailability (<20%). The objective of the present study was to increase ROS bioavailability by formulating nanosponges.
Materials and Methods
Important quality features were identified using the Quality by Design (QbD) method. Central Composite Design (CCD) was utilized to design formulations. Eudragit L-100 (EL-100) and Polyvinyl Alcohol (PVA) were used as polymers and surfactants, respectively. Nanosponges were produced using emulsion solvent evaporation (RF1-RF15). The final formulations were assessed based on parameters including drug-excipient interaction, particle size, surface morphology, Entrapment Efficiency (%EE), and in vitro drug release. The Design Expert-13 (DOE) produced the optimized Formulation (RF16), which was utilized in the in vivo drug release
Results
All Formulations (RF1-RF15) showed particle size of 99±0.84 nm to 305±0.26 nm, %EE 17.8±0.42 to 84.69±0.45, and drug release was 94.33±0.45% to 99.77±0.56% in 4 hr. Optimized Formulation (RF16) showed a particle size of 295±0.35 nm, % EE of 78.54±0.26 %, and drug release study of 95.13±0.63% in 3.5 hr. The in vivo studies showed Cmax Tmax, AUC0-t, AUC0-α, MRT0-α of the pure drug and RF16 of 7.123μg/mL and 14.787 μg/mL, 1.5 and 2.5 hr, 19.56 μg/mL*hr and 25.71 μg/ mL*hr, 23.91 μg/ml*h, and 48.85 μg/mL*hr, 5.04 hr and 3.91 hr, respectively.
Conclusion
The pharmacokinetic parameters RF16 demonstrate a 2-fold enhancement in the bioavailability of ROS nanosponges compared to the pure drug.