AmbioPharm, Inc., 1024 Dittman Court, North Augusta, South Carolina 29842.
Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John's University, Queens, New York 11439.
J Pharm Sci. 2018 Aug;107(8):2198-2207. doi: 10.1016/j.xphs.2018.03.024. Epub 2018 Apr 4.
The study aims to elucidate the mechanism and the role of the molecular structure of surfactants and lipids in the formation of oil-in-water (o/w) self-emulsified nanoemulsions (SENs). The hypothesis is that the overall change of Gibb's free energy (ΔG) during the mixing of the lipid and surfactant, the formation of the interface between the lipid nanodroplets and water, and the dispersion of the lipid nanodroplets into the water are the determinants of the formation of SEN, which are the result of the intermolecular interactions between the excipients involved. Various lipids and surfactants of different structures were studied for the possible formation of SEN. The results demonstrate that the formation of SEN requires (1) enough hydrophobic attractions between the surfactant molecule and the lipid molecule, which can break up the lipid-lipid and surfactant-surfactant intermolecular binding forces and (2) the surfactant to be able to associate with enough water molecules which can effectively cover the lipid droplets' surface to prevent coalescence.
本研究旨在阐明表面活性剂和脂质的分子结构在形成油包水(o/w)自乳化纳米乳剂(SEN)中的作用和机制。假设是脂质和表面活性剂混合过程中吉布斯自由能(ΔG)的总体变化、脂质纳米液滴与水之间界面的形成以及脂质纳米液滴在水中的分散是形成 SEN 的决定因素,这是涉及辅料之间分子相互作用的结果。研究了不同结构的各种脂质和表面活性剂,以探讨可能形成 SEN 的条件。结果表明,形成 SEN 需要(1)表面活性剂分子和脂质分子之间足够的疏水力,这可以打破脂质-脂质和表面活性剂-表面活性剂分子间的结合力,以及(2)表面活性剂能够与足够的水分子结合,这些水分子可以有效地覆盖脂质液滴的表面,以防止聚集。