Faculty Collaboration Database

Dendrimer-mediated transdermal delivery: enhanced bioavailability of indomethacin. J Control Release 2003 Jul 31;90(3):335-43

Date

07/26/2003

Pubmed ID

12880700

DOI

10.1016/s0168-3659(03)00200-1

Scopus ID

2-s2.0-0037897487 (requires institutional sign-in at Scopus site)   322 Citations

Abstract

The transdermal delivery of aqueous formulations of indomethacin, a model drug, with different concentrations of three types of dendrimer showed a linear increase in flux with increasing concentration of each of the dendrimers. This result was in contrast to phase solubility studies, where Higuchi's A(N) profile was observed. The steady-state flux of the drug increased significantly and was highest with the G4-NH2 dendrimer at 0.2% w/v concentration, which showed an enhancement factor of 4.5 compared to the pure drug suspension. In vivo, a steady-state flux was achieved in 5 h, and the C(max) values were significantly higher with G4-NH2 and G4-OH dendrimer formulations. The [AUC](0-24h) of G4-NH2 (2.27 times) and G4-OH (1.95 times) formulations were significantly higher than that of the pure drug, but was only marginally higher in the case of G-4.5 dendrimer formulation. The % inhibition of paw volume showed a trend comparable to the pharmacokinetic data and a maximum of 1.6- and 1.5-fold increase was found with G4-NH2 and G4-OH formulations, respectively, compared to the pure drug suspension.

Author List

Chauhan AS, Sridevi S, Chalasani KB, Jain AK, Jain SK, Jain NK, Diwan PV

Author

Abhay Chauhan PhD Associate Professor in the School of Pharmacy Administration department at Medical College of Wisconsin

MESH terms used to index this publication - Major topics in bold

Administration, Cutaneous
Animals
Anti-Inflammatory Agents, Non-Steroidal
Biological Availability
Chromatography, High Pressure Liquid
Indomethacin
Male
Rats
Rats, Wistar
Skin Absorption
Solubility
Time Factors