Amsalem Orit, Yuli-Amar Idit, Aserin Abraham, Garti Nissim
Casali Institute of Applied Chemistry, The Institute of Chemistry, The Hebrew University of Jerusalem, Jerusalem 91904, Israel.
Colloids Surf B Biointerfaces. 2009 Oct 1;73(1):15-22. doi: 10.1016/j.colsurfb.2009.04.020. Epub 2009 May 4.
The use of phospholipids (PL) as surfactants in micellar systems and microemulsions offers many advantages as drug delivery vehicles. PL are commonly used in combination with other non-food surfactants with cosolvents and cosurfactants to form a cascade of delivery structures. In this work, we incorporated phosphatidylcholine (PC) in our unique U-type water-dilutable phase diagrams exhibiting large isotropic regions of nanostructures. The nanometric liquid structures were prepared from food-grade emulsifiers. We formed water-free concentrates with PC that are fully diluted with water to form a variety of unusually structured nanodroplets. Due to the uniqueness of their composition, the designed concentrates derived from the nature of the oil phase, type of surfactants, and cosurfactants were characterized and found to be direct micelles (rather than inverse micelles), with the surfactant headgroups convexed toward the hydrophilic phase away from the micelle's core, even in the absence of water. The concentrates tend to self-assemble upon adding water to form O/W microemulsions even with small amounts of water (water-poor compositions of 0-20 wt% water). Upon further dilution with water the swollen micelles retain the oil as the inner phase. Multi-component compositions with two types of hydrophilic surfactants were investigated. The most significant enhancement in the total isotropic region was obtained by decreasing the triacetin and PC content in the system. We explored, by varying the nature of the headgroups and the nature and length of the lipidic (lipophilic) tails of the PL, the dilution capabilities of each of the systems.
在胶束体系和微乳液中使用磷脂(PL)作为表面活性剂,作为药物递送载体具有许多优点。PL通常与其他非食品表面活性剂以及助溶剂和共表面活性剂联合使用,以形成一系列递送结构。在这项工作中,我们将磷脂酰胆碱(PC)纳入我们独特的U型水可稀释相图中,该相图展示了纳米结构的大各向同性区域。纳米级液体结构由食品级乳化剂制备。我们用PC形成无水浓缩物,将其用水完全稀释以形成各种结构异常的纳米液滴。由于其组成的独特性,源自油相性质、表面活性剂类型和共表面活性剂的设计浓缩物经过表征,发现是直接胶束(而非反相胶束),即使在没有水的情况下,表面活性剂头基也朝着远离胶束核心的亲水性相凸出。即使加入少量水(水含量为0 - 20 wt%的贫水组合物),浓缩物在加水时也倾向于自组装形成O/W微乳液。用水进一步稀释后,膨胀的胶束将油保留在内相。研究了含有两种亲水性表面活性剂的多组分组合物。通过降低体系中三醋精和PC的含量,在总各向同性区域获得了最显著的增强。我们通过改变头基的性质以及PL的脂质(亲脂性)尾部的性质和长度,探索了每个体系的稀释能力。