Dipartimento Farmaco-Chimico, Università di Messina, V.le Annunziata, 98168 Messina, Italy.
J Pharm Biomed Anal. 2012 Dec;71:214-8. doi: 10.1016/j.jpba.2012.07.034. Epub 2012 Aug 4.
Lutein, the primary carotenoid present in the central area of the retina of eye appears to be associated with the protection against age-related macular degeneration (the leading cause of blindness in older adults). Its lipophilicity and consequently its scarce water solubility (1.3×10(-9)M) represent a drawback for bioavailability. To circumvent these unfavorable characteristics, in this work lutein (Lut) have been encapsulated in amphiphilic cyclodextrin (ACyD) by following the well-established strategy of entrapping a lipophilic drug in CyD carriers. Primary face butyrate modified β-cyclodextrins (C(4:7)) form in water nanoaggregates with a average size of 250nm and a ζ-potential of about -6mV. They are able to entrap lutein at 1:6 Lut/ACyD molar ratio by yielding nanoassemblies of vesicular aspect (320nm and -8mV) such as observed by static, dynamic and electrophoretic light-scattering. UV-vis measurements revealed that electronic properties of lutein were maintained when interact with ACyD nanoaggregates. The monitoring of the entapped carotenoid leaking from ACyD nanostructures was investigated suggesting the potential of Lut/ACyD nanoassemblies in drug delivery.
叶黄素是眼睛视网膜中央区域的主要类胡萝卜素,似乎与预防年龄相关性黄斑变性(老年人失明的主要原因)有关。其亲脂性和因此导致的水溶性差(1.3×10(-9)M)是生物利用度的一个缺点。为了克服这些不利的特性,在这项工作中,叶黄素(Lut)已被包裹在两亲性环糊精(ACyD)中,遵循将亲脂性药物包埋在 CyD 载体中的既定策略。主要是丁酸修饰的β-环糊精(C(4:7)) 在水中形成平均大小为 250nm 的纳米聚集体,ζ-电位约为-6mV。它们能够以 1:6 的 Lut/ACyD 摩尔比包封叶黄素,得到囊泡状的纳米组装体(320nm 和-8mV),如静态、动态和电泳光散射所观察到的。紫外-可见测量表明,叶黄素与 ACyD 纳米聚集体相互作用时,其电子性质得以保持。还研究了从 ACyD 纳米结构中漏出的包埋类胡萝卜素的监测情况,表明 Lut/ACyD 纳米组装体在药物传递方面具有潜力。