NIMS, National Institute for Material Science, 1-1, Namiki, Tsukuba, Ibaraki 305-0044, Japan.
Smart Biomaterials Group, Biomaterials Unit, Nano-Bio Field, MANA, National Institute for Materials Science, 1-1 Namiki, Tsukuba, Ibaraki 305-0044, Japan.
J Colloid Interface Sci. 2014 Aug 15;428:57-62. doi: 10.1016/j.jcis.2014.04.037. Epub 2014 Apr 24.
This work reports the preparation of modified poly(vinyl alcohol) PVA decorated with two different hydrophobic side-arms. Each material displays various percentages of pendant oleate and cholesteryl groups. The molar amount and the difference between their respective physico-chemical contributions are able to induce size variations of the formed micelles in aqueous media. These large amphiphilic structures hold a hydrophobic core ready for the incorporation of strong hydrophobic species such as cholesterol or prednisolone, a well-known low-water soluble steroid-type drug. In the presence of a steroid derivative, the modified PVA could form smaller and dense nanoparticles loaded in their cores. The synthesis of each polymer was controlled by (1)H NMR and FT-IR spectroscopies. The size of the empty micelles and the diameter of the loaded nanoparticles were determined by dynamic light scatting (DLS) studies. The measurement of the critical micelle concentration (CMC) was carried out for each polymer sample by fluorescence probing using pyrene. The amount of cholesterol incorporated into the hydrophobic core was estimated and all binding modes between the steroids and each amphiphilic polymer were also discussed in regard to their size distribution, concentration and stability.
本工作报道了两种不同疏水侧臂修饰的聚(聚乙烯醇)(PVA)的制备。每种材料都显示出不同比例的油酸酯和胆甾醇基团。侧基摩尔量及其各自物理化学贡献的差异能够在水相介质中诱导形成胶束的尺寸变化。这些大的两亲性结构具有一个疏水核,可用于掺入胆固醇或强疏水性物质,如泼尼松龙,一种众所周知的低水溶性甾体类药物。在甾体衍生物的存在下,修饰的 PVA 可以形成更小、更密集的载药纳米颗粒。每种聚合物的合成都通过(1)H NMR 和 FT-IR 光谱进行控制。通过动态光散射(DLS)研究测定了空胶束的大小和载药纳米颗粒的直径。通过使用芘荧光探针对每个聚合物样品进行临界胶束浓度(CMC)的测量。估计了胆固醇掺入疏水核的量,并讨论了甾体与每种两亲聚合物之间的所有结合模式,以及它们的尺寸分布、浓度和稳定性。