Pharmacokinetic evaluation of oral fenofibrate nanosuspensions and SLN in comparison to conventional suspensions of micronized drug

An increasing number of newly developed drugs show bioavailability problems due to poor water solubility. Formulating the drugs as nanosuspensions may help to overcome these problems by increasing saturation solubility and dissolution velocity. In the present study the bioavailability of the poorly...

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Bibliographic Details
Published in:Advanced drug delivery reviews 2007-07, Vol.59 (6), p.419-426
Main Authors: Hanafy, A., Spahn-Langguth, H., Vergnault, G., Grenier, P., Tubic Grozdanis, M., Lenhardt, T., Langguth, P.
Format: Article
Language:English
Subjects:
Absorption
Administration, Oral
Animals
Bioavailability enhancement
Biological Availability
Computer Simulation
Fenofibrate - administration & dosage
Fenofibrate - blood
Fenofibrate - pharmacokinetics
Hypolipidemic Agents - administration & dosage
Hypolipidemic Agents - blood
Hypolipidemic Agents - pharmacokinetics
Lipids - administration & dosage
Male
Models, Biological
Nanomedicine
Nanoparticles - administration & dosage
Nanosuspension
Nanotechnology
Oral drug delivery
Rat
Rats
Rats, Wistar
Solubility
Suspensions
Tissue Distribution
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Summary:An increasing number of newly developed drugs show bioavailability problems due to poor water solubility. Formulating the drugs as nanosuspensions may help to overcome these problems by increasing saturation solubility and dissolution velocity. In the present study the bioavailability of the poorly soluble fenofibrate following oral administration was investigated in rats. Four formulations were tested: a nanosuspension type DissoCube®, one solid lipid nanoparticle (SLN) preparation and two suspensions of micronized fenofibrate as reference formulations, one suspension in sirupus simplex and a second in a solution of hydroxyethy-cellulose in physiological saline. Both colloidal drug delivery systems showed approximately two-fold bioavailability enhancements in terms of rate and extent compared to the reference formulations. No significant differences were found in AUC 0–22 h as well as in C max and t max between the two colloidal delivery systems. In conclusion, nanosuspensions may be a suitable delivery system to improve the bioavailability of drugs with low water solubility.
ISSN:0169-409X
1872-8294
DOI:10.1016/j.addr.2007.04.005