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Transdermal Penetration of Cytarabine and Its 5-O Alkyl Ester Derivatives

[ Vol. 6 , Issue. 2 ]


Lesetja J. Legoabe, Jaco C. Breytenbach, David D. N'Da and J. Wilma Breytenbach   Pages 108 - 113 ( 6 )


The purpose of this study was to synthesize and determine the in vitro transdermal penetration of cytarabine and its 5-alkyl esters and to establish a correlation, if any, with selected physicochemical properties. The n-alkyl esters were synthesized by acylation of cytarabine (1) at its pharmacophoric 5-OH. The transdermal flux values of (1) and its esters were determined in vitro using Franz diffusion cell methodology. Aqueous solubility and log D (pH 7.4) values were determined and assessed for correlation to transdermal flux. An inverse relation was observed between the water solubility (Sw) and log D values. Of all esters, (4) exhibited the highest flux value of 22.2, which is significantly different to that of the parent drug cytarabine (3.70 No trend was found between water solubility and flux values.


Transdermal penetration, cytarabine, promoiety, esters, physicochemical properties, log D. aqueous solubility, skin


Unit for Drug Research and Development, North-West University, Private Bag X 6001, Potchefstroom, 2520, South Africa.

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