The 2nd International Conference on Drug Discovery & Therapy: Dubai, February 1 - 4, 2010


Poster Presenter

In vitro Transdermal Absorption of Cytarabine and its N4-Alkylamides Derivatives
Lesetja J. Legoabe, David D. N’ Da, Jaco C. Breytenbach, Jeanetta du Plessis
South Africa

The aim of this study was to synthesize and determine the transdermal delivery of cytarabine alkylamine derivatives and assess the correlation of flux with physicochemical properties. The alkylamide derivatives of cytarabine were synthesized by acylation at N4-amino group by mixed anhydride method. The in vitro permeation studies were performed using Franz diffusion cell methodology. Furthermore, partition coefficients (n-octanol-water) and aqueous solubility of N4-alkylamide derivatives of cytarabine were determined in order to obtain information about their lipophilicity and hydrophilicity. Alkylamides (2)-(6) showed decreased hydrophilicity and increased lipophilicity. The logD values of the alkylamides were higher than that of the parent compound and increased linearly as the alkyl chain lengthened. Compound (4) showed the highest median steady-state flux (Jss) of 89.0 nmol/cm2
/h in the series, which shows a high statistical difference with the parent compound flux value (3.70 nmol/cm2/h). The prodrug approach appears to be a promising strategy for the enhancement of transdermal absorption of cytarabine.















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