Optimization of variables and assessment of in-vitro and in-vivo antihyperlipidemic activity of Eudragit RS nanoparticles containing simvastatin--颗粒学报PARTICUOLOGY

Gidwani, B., Jain, V., Joshi, V., Pandey, R. K., Shukla, S. S., & Vyas, A. (2024). Optimization of variables and assessment of in-vitro and in-vivo antihyperlipidemic activity of Eudragit RS nanoparticles containing simvastatin. Particuology, 90, 189-198. https://doi.org/10.1016/j.partic.2023.12.006

Optimization of variables and assessment of in-vitro and in-vivo antihyperlipidemic activity of Eudragit RS nanoparticles containing simvastatin

Bina Gidwani^a, Vishal Jain^b, Veenu Joshi ^c, Ravindra Kumar Pandey ^a, Shiv Shankar Shukla ^a, Amber Vyas ^b *

a Columbia Institute of Pharmacy, Raipur (C.G.), India
b University Institute of Pharmacy, Pt Ravishankar Shukla University, Raipur (C.G.), India
c Center for Basic Science and Research, Pt Ravishankar Shukla University, Raipur (C.G.), India

10.1016/j.partic.2023.12.006

Volume 90, July 2024, Pages 189-198

Received 31 May 2023, Revised 30 November 2023, Accepted 6 December 2023, Available online 21 December 2023, Version of Record 11 January 2024.

E-mail: ambervyas@gmail.com

Highlights

• Simvastatin is associated with poor solubility, first-pass metabolism, and short half-life.

• Optimization of formulation/process parameters was done through the use of variables.

• Nanoparticles were prepared by emulsification and a solvent evaporation technique.

• There was 2.93-fold decrease in total cholesterol.

• A 3.27-fold increase in triglyceride was during in-vivo study.

Abstract

Simvastatin, a BCS class II drug, is associated with poor aqueous solubility, first-pass metabolism and short half-life. In the present work, nanoparticles were prepared and evaluated. Optimization of formulation and process parameters was done through the use of independent and dependent variables. Preliminary studies were done to determine suitable range of the concentration of Eudragit polymer (10%–30%) and the ratio of drug to polymer (1:1 to 1:5) for the formation of nanoparticles by emulsification and a solvent evaporation technique. Results revealed that the mean size of nanoparticles was affected by stirring speed from 5000 RPM, 8000 RPM, and 12000 RPM. The results of increase in association efficiency and percent yield with increase in amount of drug from 100 mg, 150 mg, and 200 mg in selected range were observed. In-vitro release studies showed that two formulations possess highest initial burst and slow sustained drug release. There was 2.93-fold decrease in total cholesterol and 3.27-fold increases in triglyceride level during in-vivo study.

Graphical abstract

Keywords

Simvastatin; Eudragit RS 100; Nanoparticles; Hyperlipidemia

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