Submit Manuscript  

Article Details


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

[ Vol. 6 , Issue. 2 ]

Author(s):

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

Abstract:


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 nmol.cm-2.h-1, which is significantly different to that of the parent drug cytarabine (3.70 nmol.cm-2.h-1). No trend was found between water solubility and flux values.

Keywords:

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

Affiliation:

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



Read Full-Text article