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Nanoparticles of Lovastatin: Design, Optimization and in vivo Evaluation

Authors Gaber DA

Received 4 December 2019

Accepted for publication 18 April 2020

Published 17 June 2020 Volume 2020:15 Pages 4225—4236

DOI https://doi.org/10.2147/IJN.S241120

Checked for plagiarism Yes

Review by Single anonymous peer review

Peer reviewer comments 2

Editor who approved publication: Prof. Dr. Anderson Oliveira Lobo


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 Arabia

Correspondence: Dalia A Gaber Tel +20 1013379892
Fax +20 2 224154781
Email dr_daliaahmed@hotmail.com

Introduction: 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

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