Adnan Burhan Qader, A. Hussein
2021
Citations
0
Influential Citations
1
Citations
Quality indicators
Journal
Systematic Reviews in Pharmacy
Abstract
Background and Objective: rosuvastatin calcium is an anti-hyperlipidemic drug. It is generally employed to treat hypercholesterolemia. This drug is a class II drug in the biopharmaceutical classification system (BCS) that shows low dissolution because of its crystalline nature and, thus, the poor oral bioavailability of 20%. The main purpose of this study is to develop a solid self-nanoemulsifying drug delivery system (S-SNEDDS) of rosuvastatin calcium for enhancement of its oral bioavailability. Methods: In this study, liquid SNEDDS (L-SNEDDS) containing rosuvastatin along with garlic oil was formulated and further developed into a solid form by the spray drying technique using Aerosil 200 as a solid carrier. Ternary phase diagrams were constructed based on rosuvastatin calcium solubility analysis for optimizing the system. A mixture of garlic oil and Stepan-Mild® GCC (1:1) used as oil phase, tween 80 and PEG 400 were used as a surfactant and co-surfactant respectively. The prepared S-SNEDDS formulas were evaluated for flow properties, reconstitution properties, FTIR study, scanning electron microscopy (SEM), differential scanning calorimetry (DSC), drug content and in-vitro drug release profile. To clarify the possible improvement in pharmacokinetic behavior of rosuvastatin S-SNEDDS, plasma concentration-time curve profiles in rats after the oral administration of optimized S-SNEDDS formula (S-B4) were compared to marketed product and pure drug in suspension. Results: results showed that S-SNEDDS formulas has good flow properties and high drug content. Reconstitution properties of S-SNEDDS showed spontaneous self-nanoemulsification and no sign of phase separation. SEM photographs showed a smooth uniform surface of S-SNEDDS with less aggregation. Results of the in-vitro drug release showed that there was a great enhancement in the dissolution rate of rosuvastatin. At all-time points, it was observed that rosuvastatin plasma concentrations in rats treated with S-SNEDDS were significantly higher than those treated with the drug in suspension and marketed product. Conclusion: in conclusion, the relative bioavailability of solid self-nano emulsified formulation S-B4 was about 2.38-fold compared to the marketed product and about 3.42-fold compared to the pure drug suspension. S-SNEDDS appeared to be an interesting approach to improving problems associated with oral delivery of rosuvastatin.