Transdermal penetration of zalcitabine, lamivudine and synthesised N-acyl lamivudine ester
Breytenbach, Jaco C.
Du Plessis, Jeanetta
MetadataShow full item record
The 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
- Faculty of Health Sciences