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dc.contributor.authorBreytenbach, Jaco Corneliusen_US
dc.contributor.authorDu Plessis, Jeanettaen_US
dc.contributor.authorGerber, Minjaen_US
dc.contributor.authorHolmes, Estee-marieen_US
dc.date.accessioned2012-02-29T09:49:41Z
dc.date.available2012-02-29T09:49:41Z
dc.date.issued2010en_US
dc.identifier.citationHolmes, 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.issn1573-4064en_US
dc.identifier.urihttp://hdl.handle.net/10394/5916
dc.description.abstractThe 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.urihttp://dx.doi.org/10.2174/157340610793358873en_US
dc.description.urihttp://www.omicsonline.org/medicinal-chemistry.php
dc.description.urihttp://www.eurekaselect.com/87019/article
dc.publisherBentham Science Publishersen_US
dc.subjectDelivery system
dc.subjectPheroid™
dc.subjectskin penetration
dc.subjectStavudine
dc.subjectStavudine esters
dc.subjecttransdermal delivery
dc.titleSynthesis and transdermal penetration of stavudine-5'-estersen_US
dc.contributor.researchID11329025 - Gerber, Minja
dc.contributor.researchID10065318 - Du Plessis, Jeanetta


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