Riess J G, Krafft M P
MRI Institute, Medical Center, University of California, San Diego 92103-1990, USA.
Biomaterials. 1998 Aug;19(16):1529-39. doi: 10.1016/s0142-9612(98)00071-4.
Fluorocarbons are characterized by exceptional chemical and biological inertness, extreme hydrophobicity, lipophobicity, high gas-dissolving capacities, low surface tensions, high fluidity and spreading coefficients, high density, absence of protons, and magnetic susceptibilities comparable to that of water. These unique properties are the foundation for a range of biomedical applications. An injectable fluorocarbon-in-water emulsion is in advanced clinical trials as a temporary oxygen carrier (blood substitute) to prevent tissue hypoxia or ischemia in the surgical and critical care patient. A liquid fluorocarbon is in Phase II/III clinical trials for treatment of acute respiratory failure through liquid ventilation. Several fluorocarbon-based contrast agents for ultra-sound imaging are in various stages of clinical investigation. Multiple families of well-defined pure fluorinated surfactants have recently been synthesized. These surfactants have a modular structure which allows stepwise adjustment of their physicochemical characteristics. Their polar head group derives from polyols, sugars, aminoacids, amides, amine oxides, phosphocholine, phosphatidylcholine, etc. Fluorinated surfactants are significantly more surface-active than their hydrocarbon analogs and they display a greater tendency to self-assemble, thus forming well-ordered, stable supramolecular assemblies such as vesicles, tubules, fibers, ribbons, etc. Fluorinated amphiphiles also allowed the obtaining of a variety of stable reverse and multiple emulsions and gels. These systems are being investigated as drug delivery devices.
碳氟化合物具有卓越的化学和生物惰性、极强的疏水性、疏脂性、高气体溶解能力、低表面张力、高流动性和铺展系数、高密度、无质子以及与水相当的磁化率等特点。这些独特性质是一系列生物医学应用的基础。一种可注射的水包碳氟化合物乳液正处于高级临床试验阶段，作为一种临时氧载体（血液替代品），用于预防外科手术和重症监护患者的组织缺氧或局部缺血。一种液态碳氟化合物正处于通过液体通气治疗急性呼吸衰竭的II/III期临床试验阶段。几种用于超声成像的碳氟化合物基造影剂正处于不同的临床研究阶段。最近合成了多个系列明确的纯氟化表面活性剂。这些表面活性剂具有模块化结构，可逐步调节其物理化学特性。它们的极性头基来源于多元醇、糖、氨基酸、酰胺、氧化胺、磷酸胆碱、磷脂酰胆碱等。氟化表面活性剂比其碳氢类似物具有显著更高的表面活性，并且它们表现出更大的自组装倾向，从而形成有序、稳定的超分子聚集体，如囊泡、小管、纤维、带状物等。氟化两亲物还能制备出各种稳定的反相乳液、多重乳液和凝胶。这些体系正在作为药物递送装置进行研究。
