Adams Monica L, Lavasanifar Afsaneh, Kwon Glen S
Division of Pharmaceutical Sciences, School of Pharmacy, University of Wisconsin-Madison, 777 Highland Avenue, Madison, WI 53705-2222, USA.
J Pharm Sci. 2003 Jul;92(7):1343-55. doi: 10.1002/jps.10397.
Amphiphilic block copolymers (ABCs) have been used extensively in pharmaceutical applications ranging from sustained-release technologies to gene delivery. The utility of ABCs for delivery of therapeutic agents results from their unique chemical composition, which is characterized by a hydrophilic block that is chemically tethered to a hydrophobic block. In aqueous solution, polymeric micelles are formed via the association of ABCs into nanoscopic core/shell structures at or above the critical micelle concentration. Upon micellization, the hydrophobic core regions serve as reservoirs for hydrophobic drugs, which may be loaded by chemical, physical, or electrostatic means, depending on the specific functionalities of the core-forming block and the solubilizate. Although the Pluronics, composed of poly(ethylene oxide)-block-poly(propylene oxide)-block-poly(ethylene oxide), are the most widely studied ABC system, copolymers containing poly(L-amino acid) and poly(ester) hydrophobic blocks have also shown great promise in delivery applications. Because each ABC has unique advantages with respect to drug delivery, it may be possible to choose appropriate block copolymers for specific purposes, such as prolonging circulation time, introduction of targeting moieties, and modification of the drug-release profile. ABCs have been used for numerous pharmaceutical applications including drug solubilization/stabilization, alteration of the pharmacokinetic profile of encapsulated substances, and suppression of multidrug resistance. The purpose of this minireview is to provide a concise, yet detailed, introduction to the use of ABCs and polymeric micelles as delivery agents as well as to highlight current and past work in this area.
两亲性嵌段共聚物（ABCs）已广泛应用于从缓释技术到基因递送等众多药物应用领域。ABCs用于递送治疗剂的效用源于其独特的化学组成，其特征在于亲水嵌段与疏水嵌段通过化学键连接。在水溶液中，ABCs在临界胶束浓度或高于临界胶束浓度时通过缔合形成纳米级核/壳结构的聚合物胶束。胶束形成后，疏水核心区域充当疏水药物的储存库，根据形成核心的嵌段和被增溶物的特定功能，可通过化学、物理或静电方式加载药物。虽然由聚（环氧乙烷）-嵌段-聚（环氧丙烷）-嵌段-聚（环氧乙烷）组成的普朗尼克是研究最广泛的ABC系统，但含有聚（L-氨基酸）和聚（酯）疏水嵌段的共聚物在递送应用中也显示出巨大的潜力。由于每种ABC在药物递送方面都有独特的优势，因此有可能针对特定目的选择合适的嵌段共聚物，例如延长循环时间、引入靶向部分以及改变药物释放曲线。ABCs已用于众多药物应用，包括药物增溶/稳定化、改变包封物质的药代动力学特征以及抑制多药耐药性。本综述的目的是对ABCs和聚合物胶束作为递送剂的使用提供简洁而详细的介绍，并突出该领域当前和过去的工作。
