Effect of poly(amidoamine) (PAMAM) dendrimer on skin permeation of 5-fluorouracil.

Abstract:

:The aim of present study is to investigate the effect of poly(amidoamine) (PAMAM) dendrimer on skin permeation of 5-fluorouracil (5FU). Permeation studies were performed using excised porcine skin in a Franz diffusion cell and (14)C labeled 5FU samples were analyzed using liquid scintillation counter. Three different vehicles were used, including phosphate buffer (PB), mineral oil (MO) and isopropyl myristate (IPM). The studies were carried out by simultaneously applying the drug and dendrimer together or by pre-treating the skin with dendrimer before drug application. Simultaneous application of drug and dendrimer increased the flux of 5FU in IPM and MO, while there was no change in PB. The increased skin partitioning of dendrimer from lipophilic vehicles increased the drug solubility in skin. Pre-treatment with dendrimer increased permeability coefficient of 5FU by 4-fold in MO and 2.5-fold in IPM, while it decreased by half in PB. Skin partitioning of 5FU increased after dendrimer treatment from lipophilic vehicles. The flux increased linearly with increase in pre-treatment time. Dendrimer pre-treatment increased transepidermal water loss and decreased skin resistance. The decrease in skin resistance directly correlated to the enhancement in skin permeation of 5FU (r(2)=0.99). Overall, the study showed that dendrimer increases the skin permeation of 5FU from lipophilic vehicles mainly by altering the skin barrier.

journal_name

Int J Pharm

authors

Venuganti VV,Perumal OP

doi

10.1016/j.ijpharm.2008.05.034

subject

Has Abstract

pub_date

2008-09-01 00:00:00

pages

230-8

issue

1-2

eissn

0378-5173

issn

1873-3476

pii

S0378-5173(08)00427-4

journal_volume

361

pub_type

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