Objective: Rosuvastatin (ROS) is a class of antihyperlipidemic agents belonging to the class of statins with poor permeability, which results in low oral bioavailability, i.e. 20%. The objective of the present study was to improve the permeability and bioavailability of ROS by developing nanocochelates using naturally biocompatible phosphatidylcholine, a type of lipid which is used as Ca2+ cations for the calcification process.
Significance: For the loaded ROS, the trapping method was used to build nanocochelates to boost the intestinal permeability of phosphatidylcholine and divalent choline is a calcium chloride cationic solution.
Methods: Nine different formulations have been produced and with varying lipid and cationic solution concentrations. The formulation of nanocochelates characterized by scanning electron microscopy, particle size, and zeta potential. Permeability studies have been conducted to determine the permeability improvement property of nanocochelates. The pharmacokinetic study was performed in Wistar albino rats to determine the bioavailability enhancement potential of nanocochlelates.
Results: The concentration of optimum lipid, calcium chloride was found to be 80 mg, 200 uL respectively which improve permeability by 3.44 times as compared to the marketed formulation. The in-vitro drug release over a prolonged period i.e.12 h. Which was substantially better than the traditional formulation of tablets. Nearly five fold enhancement in bioavailability was observed in case of optimized formulation as compared to the marketed formulation (p < 0.05).
Conclusion: The findings suggest that the use of natural lipid carrier by nanocochelates of Rosuvastatin was promising drug delivery approach.
Keywords: Nanocochelates; Rosuvastatin; bioavailability; permeability; phosphatidylcholine.