Departament de Fisicoquímica, Facultat de Farmàcia, Universitat de Barcelona, 08028 Barcelona, Spain.
Pharmaceutics. 2011 Sep 14;3(3):636-64. doi: 10.3390/pharmaceutics3030636.
Bicellar systems are lipid nanostructures formed by long- and short-chained phospholipids dispersed in aqueous solution. The morphological transitions of bicellar aggregates due to temperature, composition and time variations have been revised in this work. To this end, two bicellar systems have been considered; one formed by dimyristoyl-phosphatidylcholine (DMPC) and dihexanoyl- phosphatidylcholine (DHPC) and another formed by dipalmitoyl-phosphatidylcholine (DPPC) and DHPC. The relationship between the magnetic alignment, the morphology of the aggregates and the phase transition temperature (Tm) of lipids is discussed. In general terms, the non-alignable samples present rounded objects at temperature below the Tm. Above this temperature, an increase of viscosity is followed by the formation of large elongated aggregates. Alignable samples presented discoidal objects below the Tm. The best alignment was achieved above this temperature with large areas of lamellar stacked bilayers and some multilamellar vesicles. The effect of the inclusion of ceramides with different chain lengths in the structure of bicelles is also revised in the present article. A number of physical techniques show that the bicellar structures are affected by both the concentration and the type of ceramide. Systems are able to incorporate 10% mol of ceramides that probably are organized forming domains. The addition of 20% mol of ceramides promotes destabilization of bicelles, promoting the formation of mixed systems that include large structures. Bicellar systems have demonstrated to be morphologically stable with time, able to encapsulate different actives and to induce specific effects on the skin. These facts make bicellar systems good candidates as colloidal carriers for dermal delivery. However, water dilution induces structural changes and formation of vesicular structures in the systems; stabilization strategies have been been explored in recent works and are also updated here.
双分子层囊泡系统是由长链和短链磷脂分散在水溶液中形成的脂质纳米结构。本文综述了双分子层囊泡聚集体由于温度、组成和时间变化引起的形态转变。为此,考虑了两种双分子层囊泡系统;一种由二肉豆蔻酰基磷脂酰胆碱(DMPC)和二己酰基磷脂酰胆碱(DHPC)组成,另一种由二棕榈酰基磷脂酰胆碱(DPPC)和 DHPC 组成。讨论了磁性排列、聚集体形态和脂质相变温度(Tm)之间的关系。一般来说,低于 Tm 温度下,不可对准的样品呈现出圆形物体。在高于该温度下,粘度增加后会形成大的长形聚集体。可对准的样品在 Tm 以下呈现出圆盘状物体。在高于该温度下,通过大的层状堆叠双层和一些多层囊泡实现最佳对准。本文还综述了不同链长神经酰胺在双分子层囊泡结构中包含的影响。许多物理技术表明,双分子层结构受浓度和神经酰胺类型的影响。系统能够包含 10%摩尔的神经酰胺,这些神经酰胺可能组织形成域。添加 20%摩尔的神经酰胺会促进双分子层囊泡的不稳定性,促进形成包括大结构的混合系统。双分子层囊泡系统具有随时间保持形态稳定的特性,能够包封不同的活性剂,并对皮肤产生特定的影响。这些事实使得双分子层囊泡系统成为经皮给药的胶体载体的良好候选物。然而,水稀释会引起系统中结构变化和囊泡结构的形成;最近的研究工作已经探索了稳定策略,本文也对此进行了更新。