Butt Ummara, ElShaer Amr, Snyder Lori A S, Chaidemenou Athina, Alany Raid G
Drug Discovery, Delivery and Patient Care (DDDPC) Theme, School of Pharmacy and Chemistry, Kingston University London, Penrhyn Road, Kingston upon Thames, Surrey, KT1 2EE, UK.
School of Life Sciences, Kingston University, Kingston upon Thames, KT1 2EE, UK.
Drug Deliv Transl Res. 2016 Dec;6(6):722-734. doi: 10.1007/s13346-016-0338-3.
Fatty acids (FAs) are used by many organisms as defence mechanism against virulent bacteria. The high safety profile and broad spectrum of activity make them potential alternatives to currently used topical antibiotics for the treatment of eye infections in neonates. The current study utilised a Design of Experiment approach to optimise the quantification of five fatty acids namely; lauric acid, tridecanoic acid, myristoleic acid, palmitoleic acid and α-linolenic acid. The significance of the influence of the experimental parameters such as volume of catalyst, volume of n-hexane, incubation temperature, incubation time and the number of extraction steps on derivatisation was established by statistical screening with a factorial approach. Derivatisation was confirmed using attenuated total reflectance infrared (ATR) and 1H NMR spectrum. A gas chromatographic method (GC-FID) was developed and validated according to ICH guidelines for the identification and quantification of fatty acids. The results were found to be linear over the concentration range studied with coefficient of variation greater than 0.99 and high recovery values and low intra-day and inter-day variation values for all FAs. Then, different α-linolenic acid-based microemulsions (MEs) were prepared using Tween 80 as surfactant, polyethylene glycol 400 (PEG 400) as co surfactant and water as aqueous phase. The developed GC method was used to quantify the FA content in ME formulations. The results indicated that the developed GC method is very effective to quantify the FA content in the ME formulations. The antimicrobial efficacy of FA-based MEs were tested against Staphylococcus aureus. It was concluded that the FA-based MEs have strong antimicrobial effect against S. aureus.
脂肪酸（FAs）被许多生物体用作抵御致病性细菌的防御机制。其高安全性和广谱活性使其成为目前用于治疗新生儿眼部感染的局部抗生素的潜在替代品。本研究采用实验设计方法优化了五种脂肪酸的定量分析，这五种脂肪酸分别是：月桂酸、十三烷酸、肉豆蔻油酸、棕榈油酸和α-亚麻酸。通过因子分析的统计筛选方法，确定了催化剂体积、正己烷体积、孵育温度、孵育时间和萃取步骤数等实验参数对衍生化影响的显著性。使用衰减全反射红外（ATR）和1H NMR光谱对衍生化进行了确认。根据国际人用药品注册技术协调会（ICH）指南开发并验证了一种气相色谱法（GC-FID），用于脂肪酸的鉴定和定量分析。研究结果表明，在所研究的浓度范围内结果呈线性，变异系数大于0.99，所有脂肪酸的回收率高，日内和日间变异值低。然后，以吐温80为表面活性剂、聚乙二醇400（PEG 400）为助表面活性剂、水为水相，制备了不同的基于α-亚麻酸的微乳剂（MEs）。所开发的气相色谱法用于定量分析微乳剂配方中的脂肪酸含量。结果表明，所开发的气相色谱法对于定量分析微乳剂配方中的脂肪酸含量非常有效。测试了基于脂肪酸的微乳剂对金黄色葡萄球菌的抗菌效果。得出的结论是，基于脂肪酸的微乳剂对金黄色葡萄球菌具有很强的抗菌作用。
