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 soluble fenofibrate following oral administration was investigated in rats. Four formulations were tested: a nanosuspension type DissoCube(R), 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.
Hanafy
A
A
Department of Pharmacology, Faculty of Veterinary Medicine, Kafrelsheikh University, Egypt.
Spahn-Langguth
H
H
Vergnault
G
G
Grenier
P
P
Tubic Grozdanis
M
M
Lenhardt
T
T
Langguth
P
P
D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D003198:Computer Simulation; D011345:Fenofibrate / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D000960:Hypolipidemic Agents / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D008055:Lipids / Q000008:administration & dosage; D008297:Male; D008954:Models, Biological; D053758:Nanoparticles / Q000008:administration & dosage*; D051381:Rats; D017208:Rats, Wistar; D012995:Solubility; D013535:Suspensions; D014018:Tissue Distribution
D000960:Hypolipidemic Agents; D008055:Lipids; D013535:Suspensions; D011345:Fenofibrate