Dendrimer-mediated transdermal delivery: enhanced bioavailability of indomethacin
| Autor: | N.K. Jain, Akhlesh K. Jain, Abhay Singh Chauhan, Sanjay Jain, S Sridevi, Prakash V. Diwan, Kishore B. Chalasani |
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| Rok vydání: | 2003 |
| Předmět: |
Male
Time Factors Skin Absorption Indomethacin Cmax Pharmaceutical Science Biological Availability Pharmacology Administration Cutaneous Dosage form Pharmacokinetics Indometacin In vivo Dendrimer medicine Animals Solubility Rats Wistar Chromatography High Pressure Liquid Transdermal Chemistry Anti-Inflammatory Agents Non-Steroidal Rats Nuclear chemistry medicine.drug |
| Zdroj: | Journal of controlled release : official journal of the Controlled Release Society. 90(3) |
| ISSN: | 0168-3659 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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