Synthesis and transdermal penetration of stavudine-5'-esters

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dc.contributor.author Breytenbach, Jaco Cornelius en_US
dc.contributor.author Du Plessis, Jeanetta en_US
dc.contributor.author Gerber, Minja en_US
dc.contributor.author Holmes, Estee-marie en_US
dc.date.accessioned 2012-02-29T09:49:41Z
dc.date.available 2012-02-29T09:49:41Z
dc.date.issued 2010 en_US
dc.identifier.citation Holmes, E-M. et al. 2010. Synthesis and transdermal penetration of stavudine-5'-esters. Medicinal chemistry, 6(5):271-276. [http://www.eurekaselect.com/87019/article] en_US
dc.identifier.issn 1573-4064 en_US
dc.identifier.uri http://hdl.handle.net/10394/5916
dc.description.abstract The aim of this study was to investigate the effects of different ester groups in position 5 of stavudine on the transdermal penetration with and without the use of Pheroid™ as the delivery system. Six esters were prepared by reaction of stavudine with six different acid chlorides at room temperature. Female human abdominal skin was used for in vitro penetration in Franz diffusion cells. The experimental aqueous solubility of stavudine (104.75 mg/mL) was much higher than that of the synthesized derivatives (ranging from 0.08 to 5.17 mg/mL), while the log D (octanol-buffer partition coefficient) of stavudine (-0.85) was lower than that of its derivatives (ranging from -0.41 to 3.06). The experimental transdermal flux of stavudine (6.52 μmol/cm2.h) in PBS (phosphate buffer solution) was much higher than that of any of its derivatives (0.06 – 0.23 μmol/cm2.h), while the propionyl (6.64 μmol/cm2.h) and the butyryl esters (6.87 μmol/cm2.h) had the highest transdermal flux using the Pheroid™ (0.75 – 6.87 μmol/cm2.h) system. - See more at: http://www.eurekaselect.com/87019/article#sthash.oBpP3aWu.dpuf
dc.description.uri http://dx.doi.org/10.2174/157340610793358873 en_US
dc.description.uri http://www.omicsonline.org/medicinal-chemistry.php
dc.description.uri http://www.eurekaselect.com/87019/article
dc.publisher Bentham Science Publishers en_US
dc.subject Delivery system
dc.subject Pheroid™
dc.subject skin penetration
dc.subject Stavudine
dc.subject Stavudine esters
dc.subject transdermal delivery
dc.title Synthesis and transdermal penetration of stavudine-5'-esters en_US
dc.contributor.researchID 11329025 - Gerber, Minja
dc.contributor.researchID 10065318 - Du Plessis, Jeanetta

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