International Journal of Nanomedicine (Jun 2020)
Nanoparticles of Lovastatin: Design, Optimization and in vivo Evaluation
Abstract
Dalia A Gaber1,2 1Department of Quality Control & Quality Assurance, Holding Company for Biological Products and Vaccines, Cairo, Egypt; 2Department of Pharmaceutics, College of Pharmacy, Qassim University, Buraidah, Saudi ArabiaCorrespondence: Dalia A Gaber Tel +20 1013379892Fax +20 2 224154781Email [email protected]: The aim of the study was to optimize the processing factors of precipitation–ultrasonication technique to prepare nano-sized particles of Lovastatin (LA) for enhancing its solubility, dissolution rate and in vivo bioavailability.Methods: LA nanoparticles (LANs) were prepared using precipitation–ultrasonication technique under different processing factors. LANs were characterized in terms of particle size, zeta potential and in vitro release. Stability studies at 4°C, 25°C and 40°C were conducted for optimum formulation. In addition, the in vivo bioavailability of the optimum formula was studied in comparison to a marketed product in white master rats.Results: The optimized LAN formula (LAN15) had particle size (190± 15), polydispersity index (0.626± 0.11) and a zeta potential (− 25± 1.9 mV). The dissolution study of the nanosuspensions showed significant enhancement compared with pure drug. After 50 min, only 20.12± 1.85% of LA was dissolved while 99.1± 1.09% of LA was released from LAN15. Stability studies verified that nanosuspensions at 4°C and 25°C showed higher stability with no particle growth compared to the samples studied at 40°C. In vivo studies conducted in rats verified that there was 1.45-fold enhancement of Cmax of LAN15 as compared to marketed tablets.Conclusion: Nanoparticle prepared by ultrasonication-assisted precipitation method is a promising formula for enhancing the solubility and hence the bioavailability of Lovastatin.Keywords: hyperlipidemia, HPMC, nano size, factors, antisolvent, bioavailability
