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Enhanced bioavailability and hypolipidemic activity of Simvastatin formulations by particle size engineering: Physicochemical aspects and in vivo investigations

Paper ID Volume ID Publish Year Pages File Format Full-Text
3288 162 2013 9 PDF Available
Title
Enhanced bioavailability and hypolipidemic activity of Simvastatin formulations by particle size engineering: Physicochemical aspects and in vivo investigations
Abstract

•Particle size engineering of Simvastatin was done by media milling and SCF technology.•Significant increase in solubility and decrease in crystallinity of drug was obtained.•Changes in physicochemical aspects were confirmed by DSC, XRD, TEM, solubility studies.•Nanosuspension and SCF formulations showed enhanced hypolipidemic activity in rats.•Bioavailability enhancement for SNS was 2.6 times and SCF was 1.8 times in rats.

The objective of this study was to enhance the solubility of Simvastatin by nanosizing approaches for improving its bioavailability. Nanosuspension (Sim-NS) formulated by media milling was optimized by 32 factorial design keeping the volume of milling media (X1) and surfactant concentration (X2) as independent and the particle size (Y) as dependent variable. A minimum particle size of 250.8 ± 12.6 nm was achieved. Simvastatin was also size reduced by supercritical antisolvent (SAS) method using CO2 as antisolvent, wherein particle size was reduced from 71.3 ± 0.87 μm to 16.54 ± 0.38 μm. Sim-NS showed significant increase in saturation solubility and decrease in crystallinity of the drug as compared to Simvastatin supercritical antisolvent product (Sim-SAS) and plain drug suspension. In vitro release showed increased dissolution rate of the drug for Sim-NS followed by Sim-SAS and plain drug. Pharmacodynamic evaluation in rats showed significant decrease in the total cholesterol and triglyceride levels for Sim-NS followed by Sim-SAS and plain drug. In vivo pharmacokinetics in rats showed an increase in bioavailability of Sim-NS (2.6 times) and Sim-SAS (1.8 times) compared to plain drug. Hence, particle size engineering has tremendous potential to enhance the bioavailability and hypolipidemic activity by altering physicochemical properties of the poorly water soluble drug.

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Keywords
Optimization; Absorption; Biomedical; Nanosuspension; Supercritical antisolvent process; Kinetic parameters
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Enhanced bioavailability and hypolipidemic activity of Simvastatin formulations by particle size engineering: Physicochemical aspects and in vivo investigations
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Publisher
Database: Elsevier - ScienceDirect
Journal: Biochemical Engineering Journal - Volume 79, 15 October 2013, Pages 221–229
Authors
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Subjects
Physical Sciences and Engineering Chemical Engineering Bioengineering
Get Full-Text Now
Don't Miss Today's Special Offer
Price was $35.95
You save - $31
Price after discount Only $4.95
100% Money Back Guarantee
Full-text PDF Download
Online Support
Any Questions? feel free to contact us