Predicting skin permeation-enhancing effect of fixed oils using saturated to unsaturated fatty acid ratio content

T. Adeoye-Aremu, K.T. Jaiyeoba
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Abstract

Background: Transdermal drug delivery is non-invasive and advantageous as it improves patient compliance. Objective: This study evaluated the effect of varying ratios of saturated to unsaturated fatty acids in fixed oils on the permeation of ibuprofen across pig dorsal skin. Methods: The solubility of ibuprofen in soybean oil, theobroma oil, and shea butter (fixed oils) was evaluated and in vitro skin permeation studies were conducted using Franz diffusion cells. Results: A significant difference in permeability parameters, such as flux and effective skin permeability, in the different formulations was observed. Skin permeation depended on the ratio of saturated to unsaturated fatty acids. It also depended on the type and concentration of individual saturated and unsaturated fatty acids present in the fixed oils. The skin permeation of ibuprofen increased with an increasing ratio of palmitic acid (PA) to oleic acid (OA) concentrations. The highest flux was obtained in the theobroma oil formulation, with a PA:OA ratio of 0.78. The lowest flux was obtained in the shea butter formulation, with a PA:OA ratio of 0.09. The PA:OA ratio was 0.46 in the soybean oil formulation. Conclusion: These results suggest that the ratio of saturated to unsaturated fatty acids in fixed oils could be used as a model for predicting the rate of skin permeation of drugs in oil-based formulations. Depending on the desired rate of drug permeation, different combinations of the ratio of saturated to unsaturated fatty acids can be used in formulations for transdermal delivery.
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利用饱和脂肪酸与不饱和脂肪酸的比例含量预测固定油的皮肤渗透增强效果
背景:经皮给药是一种非侵入性的给药方式,其优点是能提高患者的依从性。研究目的本研究评估了固定油中饱和脂肪酸与不饱和脂肪酸的不同比例对布洛芬在猪背皮中渗透的影响。方法:评估布洛芬在大豆油、可可脂油和乳木果油(固定油)中的溶解度,并使用弗朗兹扩散细胞进行体外皮肤渗透研究。结果显示在不同配方中,通量和有效皮肤渗透率等渗透性参数存在明显差异。皮肤渗透性取决于饱和脂肪酸与不饱和脂肪酸的比例。它还取决于固定油中各个饱和脂肪酸和不饱和脂肪酸的类型和浓度。布洛芬的皮肤渗透率随着棕榈酸(PA)和油酸(OA)浓度比例的增加而增加。可可脂油配方的通量最高,PA 与 OA 的比率为 0.78。乳木果油配方的通量最低,PA:OA 的比率为 0.09。大豆油配方中的 PA:OA 比率为 0.46。结论这些结果表明,固定油中饱和脂肪酸与不饱和脂肪酸的比例可用作油基配方中药物皮肤渗透率的预测模型。根据所需的药物渗透率,可在透皮给药配方中使用不同的饱和与不饱和脂肪酸比例组合。
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