Nanoparticles of Lovastatin: Design, Optimization and in vivo Evaluation

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 22415...

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Autor principal: Gaber DA
Formato: article
Lenguaje:EN
Publicado: Dove Medical Press 2020
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Acceso en línea:https://doaj.org/article/f50d5d3afc934004bfff550ac888260d
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Sumario: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 dr_daliaahmed@hotmail.comIntroduction: 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