Formulation and In Vivo Evaluation of Self-Nanoemulsifying Granules for Oral Delivery of a Combination of Ezetimibe and Simvastatin

Self-nanoemulsifying granules were formulated with the objective of improving the bioavailability of the ezetimibe and simvastatin when administered together. Composition of self-nanoemulsifying system (SNS) was optimized using various modified oils, surfactant, and cosurfactant mixtures. SNSs were...

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Bibliographic Details
Published in:Drug development and industrial pharmacy 2008-01, Vol.34 (12), p.1285-1296
Main Authors: Dixit, Rahul P., Nagarsenker, M. S.
Format: Article
Language:English
Subjects:
Administration, Oral
Animals
Anticholesteremic Agents - administration & dosage
Azetidines - administration & dosage
Azetidines - chemistry
Azetidines - pharmacology
Biological and medical sciences
Chemistry, Pharmaceutical
Cholesterol - blood
colloidal silicon dioxide
Emulsions
Ezetimibe
General pharmacology
hyperlipidemia
Male
Medical sciences
Microscopy, Electron, Scanning
Nanoparticles
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Rats
Rats, Sprague-Dawley
self-nanoemulsifying granules
simvastatin
Simvastatin - administration & dosage
Simvastatin - chemistry
Simvastatin - pharmacology
Solubility
X-Ray Diffraction
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Summary:Self-nanoemulsifying granules were formulated with the objective of improving the bioavailability of the ezetimibe and simvastatin when administered together. Composition of self-nanoemulsifying system (SNS) was optimized using various modified oils, surfactant, and cosurfactant mixtures. SNSs were mixed with water and resultant emulsions were characterized for mean globule size and stability. SNSs were adsorbed on hydrophilic colloidal silicon dioxide to give free-flowing self-nanoemulsifying granules. Self-nanoemulsifying granules were characterized by X-ray diffraction pattern, scanning electron microscopy, dissolution profile, and for in vivo performance in hypercholesterolemic rats. X-ray diffraction studies and scanning electron microscopy indicated loss of crystallinity and or solubilization of both drugs in the self-nanoemulsifying granules. Self-nanoemulsifying granules effected substantial increase in dissolution of the drugs as compared with pure powder of drugs. In vivo evaluation in rats showed significant decrease in the total cholesterol levels and triglyceride levels in rats as compared with positive control confirming potential of self-nanoemulsifying granules as a drug delivery system for the poorly water-soluble drugs.
ISSN:0363-9045
1520-5762
DOI:10.1080/03639040802071570