The Ratner Chair of Chemistry, Casali Institute of Applied Chemistry, The Institute of Chemistry, The Hebrew University of Jerusalem, Edmond J. Safra Campus, Givat Ram, Jerusalem 91904, Israel.
Colloids Surf B Biointerfaces. 2013 Dec 1;112:87-95. doi: 10.1016/j.colsurfb.2013.06.051. Epub 2013 Jul 10.
The role of 2nd generation polypropyleneimine (PPIG2) dendrimer in controlling the release of gallic acid (GA) as a model drug from lyotropic liquid crystal was explored. GA (0.2wt%) was solubilized in three types of mesophases: lamellar (Lα), cubic (space group of Ia3d, Q(G)), and reverse hexagonal (HII), composed of GMO and water (and d-α-tocopherol, or tricaprylin in the case of HII mesophases). Small angle X-ray scattering (SAXS) and attenuated total reflectance Fourier transform infrared (ATR-FTIR) along with UV spectrophotometry were utilized to elucidate the structure modifications and release resulting from the cosolubilization of GA and PPIG2. Solubilization of PPIG2 into Lα and Q(G) phases caused transformation of both structures to HII. The diffusion of GA out of the mesophases was found to be dependent on water content and PPIG2 concentration. Rapid release from Lα+PPIG2 and Q(G)+PPIG2 mesophases was recorded. The release from both HII mixtures (with d-α-tocopherol and tricaprylin) was shown to be dependent on the type of oil. Release studies conducted for 72h showed that GA release can be modulated and sustained by the presence of PPIG2, supposedly due to the electrostatic interactions between the dendrimer and the drug molecule.
研究了第二代聚丙稀亚胺(PPIG2)树枝状大分子在控制没食子酸(GA)从溶致液晶中释放的作用,作为模型药物。GA(0.2wt%)溶解在三种中间相:层状(Lα)、立方(空间群 Ia3d,Q(G))和反向六方(HII),由 GMO 和水(以及 HII 中间相中的 d-α-生育酚或三辛酸甘油酯组成)。小角 X 射线散射(SAXS)和衰减全反射傅里叶变换红外(ATR-FTIR)以及紫外分光光度法用于阐明由于 GA 和 PPIG2 的共溶导致的结构修饰和释放。PPIG2 溶解到 Lα和 Q(G)相中会导致这两种结构向 HII 转变。发现 GA 从中间相中的扩散取决于含水量和 PPIG2 浓度。记录到 Lα+PPIG2 和 Q(G)+PPIG2 中间相的快速释放。发现两种 HII 混合物(含 d-α-生育酚和三辛酸甘油酯)的释放都取决于油的类型。进行 72 小时的释放研究表明,PPIG2 的存在可以调节和维持 GA 的释放,这可能是由于树枝状大分子和药物分子之间的静电相互作用。