Kessel D
Department of Pharmacology, Wayne State University School of Medicine, Detroit 48201.
Photochem Photobiol. 1992 Oct;56(4):447-51. doi: 10.1111/j.1751-1097.1992.tb02187.x.
Using 1-anilino,8-naphthalenesulfonic acid (ANS) as a probe, we examined properties of micelles of Cremophor EL, an amphipathic agent which can solubilize hydrophobic photosensitizing agents and promote their distribution to plasma lipoprotein. In aqueous solution, Cremophor micelles persisted for several hours after dilution below the critical micellar concentration (CMC). After equilibrium was reached, we found a CMC of 0.009% (wt/vol). Fluorescence data suggest that the micellar environment of ANS binding has a dielectric constant of approximately 27. Cremophor also reverses examples of multi-drug resistance associated with impaired accumulation of anti-tumor agents, e.g. daunorubicin. Although the latter drug is relatively hydrophilic, fluorescence spectroscopy and anisotropy studies indicate an association with Cremophor. Moreover, resistance reversal occurred only at Cremophor concentrations above the CMC.
我们以1-苯胺基-8-萘磺酸（ANS）作为探针，研究了聚氧乙烯蓖麻油（Cremophor EL）胶束的性质。聚氧乙烯蓖麻油是一种两亲性试剂，能够增溶疏水性光敏剂并促进其向血浆脂蛋白的分布。在水溶液中，稀释至临界胶束浓度（CMC）以下后，聚氧乙烯蓖麻油胶束仍能持续存在数小时。达到平衡后，我们测得CMC为0.009%（重量/体积）。荧光数据表明，ANS结合的胶束环境的介电常数约为27。聚氧乙烯蓖麻油还能逆转与抗肿瘤药物（如柔红霉素）蓄积受损相关的多药耐药实例。尽管后一种药物相对亲水，但荧光光谱和各向异性研究表明其与聚氧乙烯蓖麻油有关联。此外，只有在聚氧乙烯蓖麻油浓度高于CMC时才会发生耐药逆转。
