School of Pharmacy, Monash University Malaysia, Jalan Lagoon Selatan, Subang Jaya, Malaysia.
Fatima College of Health Sciences, Al Ain, United Arab Emirates.
J Liposome Res. 2021 Sep;31(3):217-229. doi: 10.1080/08982104.2020.1777155. Epub 2020 Aug 30.
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 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. 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.
鸵鸟油具有抗炎特性,且能够作为渗透增强剂,因此它是一种理想的用于经皮制剂的药物。本研究旨在开发一种有效的 4-羟基他莫昔芬(4-OHT)传递体,4-OHT 是一种抗癌药物,使用鸵鸟油作为载体来治疗乳腺癌(BC)。使用大豆卵磷脂和三种不同的边缘活性剂(EAs),通过旋转蒸发-超声法,在五个不同的摩尔比下制备含鸵鸟油和不含鸵鸟油的 4-OHT 传递体。通过物理化学特性和研究选择最佳传递体配方。研究发现,牛磺胆酸钠是最适合的 EA,其在 85:15(w/w)摩尔比下的包封效率最高,为 95.1±2.70%,在 75:25(w/w)摩尔比下的囊泡粒径最小,为 82.3±0.02nm。TEM 和 DSC 研究表明,囊泡很容易识别,呈近乎完美的球形。此外,含有鸸鹋油的配方比含有鸵鸟油的配方更稳定。4°C 下的物理稳定性研究表明,鸵鸟油传递体在 4 周内稳定,而不含鸵鸟油的传递体在 8 周内稳定。使用猪皮进行的渗透性研究表明,含有(85:15,w/w)且不含鸸鹋油的 4-OHT 传递体配方具有增强 4-OHT 渗透的潜力,这可能有益于治疗 BC。