Sawant Rupa R, Torchilin Vladimir P
Department of Pharmaceutical Sciences and Center for Pharmaceutical Biotechnology and Nanomedicine, Northeastern University, Boston, MA, USA.
Methods Mol Biol. 2010;624:131-49. doi: 10.1007/978-1-60761-609-2_9.
One of the renowned nanosized pharmaceutical carriers for delivery of poorly soluble drugs, especially, in cancer, is micelles, which are self-assembled colloidal particles with a hydrophobic core and hydrophilic shell. Among the micelle-forming compounds, micelles made of polyethylene glycol-phosphatidylethanolamine (PEG-PE) have gained more attention due to some attractive properties such as good stability, longevity, and ability to accumulate in the areas with an abnormal vasculature via the enhanced permeability and retention effect (into the areas with leaky vasculature, such as tumors). Additionally these micelles can be made "targeted" by attaching specific targeting ligand molecules to the micelle surface or can be comprised of stimuli-responsive amphiphilic block copolymers. Addition of second component such as surfactant or another hydrophobic material to the main micelle forming material further improves the solubilizing capacity of micelles without compromising their stability. Micelles carrying various contrast agents may become the imaging agents of choice in different imaging modalities. Here, we have discussed various protocols for preparation and evaluation of PEG-PE-based micelles.
作为用于递送难溶性药物（尤其是癌症药物）的著名纳米级药物载体之一，胶束是具有疏水核心和亲水外壳的自组装胶体颗粒。在形成胶束的化合物中，由聚乙二醇 - 磷脂酰乙醇胺（PEG-PE）制成的胶束因其具有一些吸引人的特性而受到更多关注，例如稳定性好、寿命长以及能够通过增强的渗透和滞留效应（进入血管渗漏的区域，如肿瘤）在血管异常的区域积累。此外，这些胶束可以通过将特定的靶向配体分子连接到胶束表面而制成“靶向”胶束，或者可以由刺激响应性两亲嵌段共聚物组成。在主要的胶束形成材料中添加第二组分（如表面活性剂或另一种疏水材料）可进一步提高胶束的增溶能力，同时不影响其稳定性。携带各种造影剂的胶束可能成为不同成像模式下的首选成像剂。在此，我们讨论了基于PEG-PE的胶束的各种制备和评估方案。
