Preparation, characterization, and in vitro and in vivo evaluation of lovastatin solid lipid nanoparticles

The purpose of this research was to study whether the bioavailability of lovastatin could be improved by administering lovastatin solid lipid nanoparticles (SLN) duodenally to rats. Lovastatin SLN were developed using triglycerides by hot homogenization followed by ultrasonication. Particle size and...

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Bibliographic Details
Published in:AAPS PharmSciTech 2007-03, Vol.8 (1), p.24-E170
Main Authors: Suresh, G, Manjunath, K, Venkateswarlu, V, Satyanarayana, V
Format: Article
Language:English
Subjects:
Animals
Anticholesteremic Agents - administration & dosage
Anticholesteremic Agents - blood
Anticholesteremic Agents - chemistry
Anticholesteremic Agents - pharmacokinetics
Capsules - chemistry
Delayed-Action Preparations - administration & dosage
Delayed-Action Preparations - chemistry
Delayed-Action Preparations - pharmacokinetics
Diffusion
Drug Carriers - chemistry
Drug Compounding - methods
Drug Evaluation, Preclinical
Lipids - chemistry
Liposomes - chemistry
Lovastatin - administration & dosage
Lovastatin - blood
Lovastatin - chemistry
Lovastatin - pharmacokinetics
Male
Materials Testing
Nanoparticles - chemistry
Particle Size
Powders
Rats
Rats, Wistar
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Summary:The purpose of this research was to study whether the bioavailability of lovastatin could be improved by administering lovastatin solid lipid nanoparticles (SLN) duodenally to rats. Lovastatin SLN were developed using triglycerides by hot homogenization followed by ultrasonication. Particle size and zeta potential were measured by photon correlation spectroscopy. The solid state of the drug in the SLN and lipid modification were characterized. Bioavailability studies were conducted in male Wistar rats after intraduodenal administration of lovastatin suspension and SLN. Stable lovastatin SLN having a mean size range of 60 to 119 nm and a zeta potential range of -16 to -21 mV were developed. More than 99% of the lovastatin was entrapped in the SLN. Lovastatin was dispersed in an amorphous state, and triglycerides were in beta(1) form in the SLN. In vitro stability studies showed the slow release and stability of lovastatin SLN. The relative bioavailabilities of lovastatin and lovastatin hydroxy acid of SLN were increased by ~173% and 324%, respectively, compared with the reference lovastatin suspension.
ISSN:1530-9932
1530-9932
DOI:10.1208/pt0801024