Department of Pharmaceutics, Utrecht Institute for Pharmaceutical Sciences (UIPS), Utrecht University, P.O. Box 80082, 3508 TB Utrecht, The Netherlands.
Adv Drug Deliv Rev. 2010 Feb 17;62(2):231-9. doi: 10.1016/j.addr.2009.11.029. Epub 2009 Dec 22.
Polymeric micelles have been under extensive investigation during the past years as drug delivery systems, particularly for anticancer drugs. They are formed by the self-assembly of amphiphilic block copolymers in aqueous solutions and have a spherical shape and a size in the nano-range (<200nm). Tumor accumulation of polymeric micelles upon intravenous administration can occur as a result of the leaky vasculature of tumor tissue (called the enhanced permeation and retention (EPR) effect).To benefit from the EPR effect, polymeric micelles need to have prolonged circulation times as well as high and stable drug loadings. Poly[N-(2-hydroxypropyl) methacrylamide] (pHPMA) is a hydrophilic polymer currently under investigation for its use in polymer-drug conjugates. Its biocompatibility, non-immunogenicity and the possibility for functionalization are properties that resulted in broad pharmaceutical and biomedical applications, also in the micelle technology research. Being hydrophilic, it can serve as a micellar stealth corona, while it can also be modified with hydrophobic moieties to serve as a micellar core in which hydrophobic drugs can be solubilized and retained. HPMA-based polymeric micelles have been showing very promising in vitro and in vivo results. This review summarizes the applications of pHPMA in the field of polymeric micelles, either serving as a micellar stealth corona, or, if hydrophobically rendered by derivatization, as a micellar core.
高分子胶束作为药物传递系统，尤其是抗癌药物的传递系统，在过去几年中受到了广泛的研究。它们是由两亲性嵌段共聚物在水溶液中自组装形成的，具有球形和纳米级尺寸（<200nm）。静脉给药后，高分子胶束在肿瘤组织中的积累是由于肿瘤组织的血管渗漏（称为增强渗透和保留（EPR）效应）。为了受益于 EPR 效应，高分子胶束需要具有延长的循环时间以及高且稳定的药物载量。聚[N-（2-羟丙基）甲基丙烯酰胺]（pHPMA）是一种亲水性聚合物，目前正在研究其用于聚合物-药物偶联物。其生物相容性、非免疫原性和功能化的可能性是导致其在广泛的药物和生物医学应用中，以及在胶束技术研究中的应用的特性。由于其亲水性，它可以作为胶束的隐形冠，同时也可以用疏水性部分进行修饰，作为胶束的核心，其中可以溶解和保留疏水性药物。基于 HPMA 的高分子胶束在体外和体内都表现出非常有前途的结果。本综述总结了 pHPMA 在高分子胶束领域的应用，无论是作为胶束的隐形冠，还是通过衍生化为疏水性胶束核心。
