Abstract

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 (4-OHT), an anti-cancer drug, using ratite oil as a carrier agent for the treatment of breast cancer (BC). The 4-OHT transfersomes were prepared with and without ratite oils using soy phosphatidylcholine and three different edge activators (EAs) 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 characterization of the developed formulations found sodium taurocholate to be the most suitable EA, which recorded highest entrapment efficiency of 95.1 ± 2.70% with 85:15, (w/w) and lowest vesicle size of 82.3 ± 0.02 nm with 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-OHT 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-OHT, which may be beneficial in the treatment of BC.

摘要

平胸油的抗炎特性及其作为渗透促进剂的能力使其成为用于透皮制剂的理想药剂。本研究旨在开发一种有效的传递体传递 4-羟基三苯氧胺 (4-OHT)，一种抗癌药物，使用平胸油作为治疗乳腺癌 (BC) 的载体剂。使用大豆磷脂酰胆碱和三种不同的边缘活化剂 (EA) 以五种不同的摩尔比，使用旋转蒸发 - 超声方法制备 4-OHT 转移体，有和没有平胸油。使用物理化学表征和离体选择最佳传递体配方学习。所开发制剂的物理化学表征结果发现牛磺胆酸钠是最合适的 EA，其包封率最高为 95.1 ± 2.70%，85:15 (w/w)，最低囊泡尺寸为 82.3 ± 0.02 nm， 75:25，(w/w) 摩尔比。TEM 和 DSC 研究表明，囊泡很容易被识别并以近乎完美的球形存在。此外，鸸鹋油配方比鸵鸟油配方具有更好的稳定性。4 °C 下的物理稳定性研究表明，平胸油传递体可稳定长达 4 周，而不含平胸油的传递体可稳定 8 周。离体 使用猪皮的渗透性研究得出结论，不含鸸鹋油的 4-OHT 传递体制剂（85:15，w/w）有可能用于透皮给药方法，以增强 4-OHT 的渗透，这可能有益于治疗不列颠哥伦比亚省。