Preparation and characterization of nanocochelate by using phosphatidylcholine as lipid carrier for enhancement of permeability and bioavailability of rosuvastatin

Abstract

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.

GRAPHICAL ABSTRACT

Keywords:

• Nanocochelates
• phosphatidylcholine
• Rosuvastatin
• permeability
• bioavailability

Acknowledgments

Authors are thankful to Dr. R.S Bhambar; Principal, MGV’S Pharmacy College, Panchavati, Nashik, Maharashtra State, India –422 003 for providing best of the facility to conduct this research work.

Disclosure statement

No potential conflict of interest was reported by the author(s).

Funding

The author(s) reported there is no funding associated with the work featured in this article.

Data availability statement

The data that support the findings of this study are available on request from the corresponding author.