Torchilin Vladimir P
Department of Pharmaceutical Sciences, School of Pharmacy, Bouve College of Health Sciences, Northeastern University, 360 Huntington Avenue, Boston, MA 02115, USA.
Adv Drug Deliv Rev. 2002 Feb 21;54(2):235-52. doi: 10.1016/s0169-409x(02)00019-4.
The review deals with the fast growing field of diagnostic micelles. The need and requirements for microparticulate contrast agents are discussed. Brief analysis of the micellization process and micelle properties shows that micelles made of amphiphilic co-polymers seem to be the most attractive for practical application. These micelles can be prepared from the variety of co-polymers including hydrophilic polymers grafted on one terminus with lipid residues. Polymeric micelles are considered loaded or modified with various contrast reporter moieties for gamma-scintigraphy, magnetic resonance imaging (MRI), and computed tomography (CT). Their in vitro and in vivo properties are discussed and the results of the initial animal experiments are presented. Mixed micelles were prepared from diacyllipid-polyethylene glycol (PEG) conjugates and polymeric amphiphilic chelates, containing entrapped metals, such as 111-In or Gd, and used for the experimental gamma- and MR imaging of various components of lymphatic system in rabbits. The method is also described to prepare polymeric iodine-containing PEG-based micelles which may act as a long-circulating blood pool imaging agent for CT. Experimental CT-imaging performed in mice and rabbits demonstrated high potential of a micellar contrast agent.
本综述涉及快速发展的诊断性胶束领域。讨论了微粒造影剂的需求和要求。对胶束化过程和胶束性质的简要分析表明，由两亲性共聚物制成的胶束在实际应用中似乎最具吸引力。这些胶束可以由多种共聚物制备，包括在一端接有脂质残基的亲水性聚合物。聚合物胶束被认为用各种造影剂标记部分进行了负载或修饰，用于γ闪烁显像、磁共振成像（MRI）和计算机断层扫描（CT）。讨论了它们的体外和体内性质，并展示了初步动物实验的结果。混合胶束由双酰基脂质 - 聚乙二醇（PEG）缀合物和含有包封金属（如¹¹¹In或Gd）的聚合物两亲螯合物制备而成，并用于兔子淋巴系统各组分的实验性γ和MR成像。还描述了制备基于含碘PEG的聚合物胶束的方法，其可作为用于CT的长循环血池显像剂。在小鼠和兔子身上进行的实验性CT成像证明了胶束造影剂的巨大潜力。
