Gómez Gaete Carolina, Tsapis Nicolas, Silva Lídia, Bourgaux Claudie, Fattal Elias
Univ Paris Sud, UMR CNRS 8612, Faculté de Pharmacie, Châtenay-Malabry, France.
Eur J Pharm Sci. 2008 May 10;34(1):12-21. doi: 10.1016/j.ejps.2008.02.003. Epub 2008 Feb 15.
We characterized the morphology, structure and supramolecular organization of microparticles obtained by spray drying 1,2-dipalmitoyl-sn-glycero-3-phosphatidylcholine (DPPC) and hyaluronic acid (HA). Pure DPPC microparticles are small and strongly aggregated with phospholipids organized in a lamellar-like structure observable by scanning electron microscopy (SEM). X-ray scattering demonstrates that it corresponds to an almost dry lamellar phase with chains tilted with respect to the bilayer surface and organized according to a hexagonal lattice within the bilayer. Upon aging, DPPC reorganizes into an orthorhombic structure within the bilayer. The addition of HA leads to an increase of particle size and a decrease of aggregation and tap density associated to a morphology switch from dense spheres to hollow shells. By contrast, the supramolecular organization is not modified: HA is mostly "sandwiched" between DPPC headgroups. In addition, HA impedes phospholipids rearrangement upon aging. Altogether, for drug delivery purposes, the addition of HA is beneficial in terms of stability and physical properties.
我们对通过喷雾干燥1,2-二棕榈酰-sn-甘油-3-磷酸胆碱(DPPC)和透明质酸(HA)得到的微粒的形态、结构和超分子组织进行了表征。纯DPPC微粒很小,且强烈聚集,通过扫描电子显微镜(SEM)可观察到磷脂以层状结构排列。X射线散射表明,它对应于一个几乎干燥的层状相,链相对于双层表面倾斜,并在双层内按六方晶格排列。老化后,DPPC在双层内重新组织成正交结构。HA的加入导致粒径增加,聚集和振实密度降低,同时形态从致密球体转变为空心壳。相比之下,超分子组织未被改变:HA大多“夹在”DPPC头基之间。此外,HA阻碍老化过程中磷脂的重排。总体而言,就药物递送目的而言,HA的加入在稳定性和物理性质方面是有益的。