Ratite oils for local transdermal therapy of 4-OH Tamoxifen: Development, Characterization and Ex-vivo Evaluation.

The anti-inflammatory property of ratite oils as well as its ability to act as a penetration enhancer makes it an ideal agent to be used in transdermal formulations. The present study aims to develop an effective transfersomal delivery of 4-hydroxytamoxifen, an anti-cancer drug, using ratite oil as a carrier agent for the treatment of breast cancer. The 4-hydroxytamoxifen transfersomes were prepared with and without ratite oils using soy phosphatidylcholine and three different edge activators in five different molar ratios using the rotary evaporation-ultrasonication method. Optimal transfersome formulations were selected using physical-chemical characterization and ex vivo studies. Results from physical-chemical characterisation of the developed formulations found sodium taurocholate to be the most suitable edge activator, whichrecorded highest entrapment efficiency of 95.1 ± 2.70% with 85:15, (w/w) and lowest vesicle size of 82.3 ± 0.02 nmwith 75:25, (w/w) molar ratios. TEM and DSC studies showed that the vesicles were readily identified and present in a nearly perfect spherical shape. In addition, formulations with emu oil had better stability than formulations with ostrich oil. Physical stability studies at 4 °C showed that ratite oil transfersomes were stable up to 4 weeks, while transfersomes without ratite oils were stable for 8 weeks. Ex vivo permeability studies using porcine skin concluded that 4-hydroxytamoxifen transfersomal formulations with (85:15, w/w) without emu oil have the potential to be used in transdermal delivery approach to enhance permeation of 4-hydroxytamoxifen, which may be beneficial in the treatment of breast cancer.