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dc.contributor.authorGerber, Minja
dc.contributor.authorBreytenbach, Jaco C.
dc.contributor.authorDu Plessis, Jeanetta
dc.identifier.citationGerber, M. et al. 2008. Transdermal penetration of zalcitabine, lamivudine and synthesised N-acyl lamivudine esters. International journal of pharmaceutics, 351(1-2):186-193. []en
dc.description.abstractThe objective of this study was to determine the in vitro transdermal permeation through human epidermis of zalcitabine, lamivudine and the synthesised N-acyl lamivudine esters, with and without the use of Pheroid™ as delivery system and to establish a correlation, if any, with selected physicochemical properties. Six N-acyl lamivudine esters were prepared by acylation of lamivudine with six different acid chlorides. The experimental aqueous solubility, log D and in vitro transdermal flux values were determined for these compounds. There was an inverse correlation between the aqueous solubility and the log D values. The median flux of zalcitabine (0.442 μmol/cm2 h) in PBS was lower than that of lamivudine (4.289 μmol/cm2 h), but in Pheroid™, lamivudine (0.011 μmol/cm2 h) had a slightly lower median flux than zalcitabine (0.015 μmol/cm2 h). Entrapment of compounds in Pheroid was confirmed by confocal laser scanning microscopy
dc.subjectN-acyl lamivudine esters
dc.subjectSkin penetration
dc.subjectTransdermal delivery
dc.titleTransdermal penetration of zalcitabine, lamivudine and synthesised N-acyl lamivudine esteren
dc.contributor.researchID10059768 - Breytenbach, Jaco Cornelius
dc.contributor.researchID10065318 - Du Plessis, Jeanetta
dc.contributor.researchID11329025 - Gerber, Minja

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