Department of Chemistry, Tulane University, New Orleans Louisiana 70118, United States.
Biomacromolecules. 2011 Apr 11;12(4):898-906. doi: 10.1021/bm101185t. Epub 2011 Feb 22.
Amphiphilic star polymers offer substantial promise for a range of drug delivery applications owing to their ability to encapsulate guest molecules. One appealing but underexplored application is transdermal drug delivery using star block copolymer reverse micelles as an alternative to the more common oral and intravenous routes. We prepared 6- and 12-arm amphiphilic star copolymers via atom transfer radical polymerization (ATRP) of sequential blocks of polar oligo (ethylene glycol)methacrylate and nonpolar lauryl methacrylate from brominated dendritic macroinitiators based on 2,2-bis(hydroxymethyl) propionic acid. These star block copolymers demonstrate the ability to encapsulate polar dyes such as rhodamine B and FITC-BSA in nonpolar media via UV/vis spectroscopic studies and exhibit substantially improved encapsulation efficiencies, relative to self-assembled "1-arm" linear block copolymer analogs. Furthermore, their transdermal carrier capabilities were demonstrated in multiple dye diffusion studies using porcine skin, verifying penetration of the carriers into the stratum corneum.
两亲性星型聚合物因其能够包裹客体分子，在一系列药物传递应用中具有巨大的应用潜力。一种吸引人但尚未充分探索的应用是使用星型嵌段共聚物反向胶束作为更常见的口服和静脉途径的替代物进行透皮药物传递。我们通过原子转移自由基聚合（ATRP），从基于 2,2-双（羟甲基）丙酸的溴化树枝状大分子引发剂上的顺序块聚极性的寡（乙二醇）甲基丙烯酸酯和非极性的月桂基甲基丙烯酸酯，制备了 6 臂和 12 臂两亲性星型共聚物。这些星型嵌段共聚物通过紫外/可见光谱研究证明了在非极性介质中包裹极性染料（如罗丹明 B 和 FITC-BSA）的能力，并表现出相对自组装的“1 臂”线性嵌段共聚物类似物显著提高的封装效率。此外，通过使用猪皮进行的多项染料扩散研究证明了它们作为透皮载体的能力，验证了载体渗透到角质层。
