Sharma Praveen K, Reilly Meghan J, Jones Deanna N, Robinson Paul M, Bhatia Surita R
Department of Chemical Engineering, 159 Goessmann Laboratory, University of Massachusetts, Amherst, MA 01003-9303, USA.
Colloids Surf B Biointerfaces. 2008 Jan 15;61(1):53-60. doi: 10.1016/j.colsurfb.2007.07.002. Epub 2007 Jul 19.
We present results on the effects of various hydrophobic drugs and additives on the micellar structure of Pluronic F127 solutions. Small-angle neutron scattering experiments on 5wt% F127 solutions were used to measure micelle core size (R(1)), micelle corona size (R(2)), intermicellar interaction distance (R(int)), polydispersity (sigma), and aggregation number (N(agg)); dynamic light scattering was used to measure critical micelle concentration (CMC); and ultraviolet spectroscopy was used to measure drug solubility and apparent micelle-water partition coefficient (K(mw)). The core and corona size were found to generally increase in the presence of the drugs, as did R(int). Both sigma and N(agg) were found to decrease in the presence of most of the drugs, and the CMC was found to vary considerably with no clear correlation. A design of experiments (DOE) approach was used to analyze the results and build empirical correlations. All of the parameters from the SANS experiments were found to depend strongly on drug solubility, with a weak dependence on K(mw) in most cases. The aggregation number, however, was found to depend strongly on both K(mw) and solubility. The correlations can be used to roughly predict the structural parameters of F127 micelles for other hydrophobic drugs.
我们展示了各种疏水性药物和添加剂对泊洛沙姆F127溶液胶束结构影响的结果。对5wt% F127溶液进行小角中子散射实验,以测量胶束核尺寸(R(1))、胶束冠尺寸(R(2))、胶束间相互作用距离(R(int))、多分散性(sigma)和聚集数(N(agg));动态光散射用于测量临界胶束浓度(CMC);紫外光谱用于测量药物溶解度和表观胶束-水分配系数(K(mw))。发现药物存在时,核尺寸和冠尺寸通常会增加,R(int)也是如此。发现大多数药物存在时,sigma和N(agg)都会降低,并且发现CMC变化很大,没有明显的相关性。采用实验设计(DOE)方法分析结果并建立经验相关性。发现小角中子散射实验的所有参数都强烈依赖于药物溶解度,在大多数情况下对K(mw)的依赖性较弱。然而,发现聚集数强烈依赖于K(mw)和溶解度。这些相关性可用于大致预测其他疏水性药物的F127胶束的结构参数。