Gerber, MinjaBreytenbach, Jaco C.Du Plessis, Jeanetta2010-02-022010-02-022008Gerber, M. et al. 2008. Transdermal penetration of zalcitabine, lamivudine and synthesised N-acyl lamivudine esters. International journal of pharmaceutics, 351(1-2):186-193. [https://doi.org/10.1016/j.ijpharm.2007.09.040]0378-5173http://hdl.handle.net/10394/2784https://www.sciencedirect.com/science/article/pii/S0378517307008198https://doi.org/10.1016/j.ijpharm.2007.09.040The 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 microscopyenZalcitabineLamivudineN-acyl lamivudine estersSkin penetrationTransdermal deliveryArticle