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Maintaining Hydrophobic Drug Supersaturation in a Micelle Corona Reservoir
Macromolecules ( IF 5.1 ) Pub Date : 2018-01-03 00:00:00 , DOI: 10.1021/acs.macromol.7b02297 Ziang Li 1 , Theodore I. Lenk 1 , Letitia J. Yao 1 , Frank S. Bates 1 , Timothy P. Lodge 1
Macromolecules ( IF 5.1 ) Pub Date : 2018-01-03 00:00:00 , DOI: 10.1021/acs.macromol.7b02297 Ziang Li 1 , Theodore I. Lenk 1 , Letitia J. Yao 1 , Frank S. Bates 1 , Timothy P. Lodge 1
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Two poly(N-isopropylacrylamide-co-N,N-dimethylacrylamide) (PND) statistical copolymers and a series of three poly(N-isopropylacrylamide-co-N,N-dimethylacrylamide)-b-polystyrene (PND-b-PS-C12) diblock polymers were synthesized by reversible addition–fragmentation chain transfer (RAFT) polymerization, in which the molecular weight of the thermoresponsive PND corona block was held constant while the polystyrene core block length was varied. The corona thickness and density of the micelles in phosphate-buffered saline (PBS, pH = 6.5) were quantified by a combination of dynamic light scattering (DLS) and small-angle X-ray scattering (SAXS). Two hydrophobic model drugs, phenytoin and nilutamide, were used to examine the drug–polymer interactions in aqueous solution. Intermolecular interactions between the diblock polymer micelle corona and both drugs were revealed by 2D 1H nuclear Overhauser effect spectroscopy (NOESY). The drug–polymer “binding” strength, quantified by diffusion ordered NMR spectroscopy (DOSY), increased as corona density of the diblock polymer micelle increased for both drugs. The in vitro dissolution of the amorphous solid dispersions was systematically investigated as a function of drug type, drug loading, and the solution-state assembly of the polymers by using either a selective or nonselective spray drying solvent. Forming micelles prior to spray drying significantly enhanced phenytoin dissolution and supersaturation maintenance for the diblock polymers by storing the drug molecules in the corona.
中文翻译：
在Micelle电晕水库中维持疏水性药物过饱和
两个聚（Ñ -isopropylacrylamide-共- Ñ，Ñ二甲基丙烯酰胺）（PND）统计共聚物和三个系列的聚（Ñ -isopropylacrylamide-共- Ñ，Ñ二甲基丙烯酰胺） - b -聚苯乙烯（PND- b -PS- C 12）二嵌段聚合物是通过可逆加成-断裂链转移（RAFT）聚合反应合成的，其中热响应性PND电晕嵌段的分子量保持恒定，而聚苯乙烯核心嵌段的长度却有所变化。通过动态光散射（DLS）和小角度X射线散射（SAXS）的组合来定量磷酸盐缓冲液（PBS，pH = 6.5）中胶束的电晕厚度和密度。两种疏水性模型药物苯妥英钠和尼鲁米特用于检查水溶液中药物与聚合物的相互作用。2D 1显示了二嵌段聚合物胶束电晕与两种药物之间的分子间相互作用H核Overhauser效应光谱（NOESY）。随着两种药物的二嵌段聚合物胶束电晕密度的增加，通过扩散有序NMR光谱法（DOSY）量化的药物-聚合物“结合”强度也增加了。在体外的无定形固体分散体的溶解系统的研究药物类型的函数，载药量，并且将溶液状态的组件的聚合物的通过使用一个选择性或非选择性喷雾干燥溶剂。通过将药物分子储存在电晕中，在喷雾干燥之前形成胶束可显着提高苯妥英溶解和二嵌段聚合物的过饱和度。
更新日期：2018-01-03
中文翻译：
在Micelle电晕水库中维持疏水性药物过饱和
两个聚（Ñ -isopropylacrylamide-共- Ñ，Ñ二甲基丙烯酰胺）（PND）统计共聚物和三个系列的聚（Ñ -isopropylacrylamide-共- Ñ，Ñ二甲基丙烯酰胺） - b -聚苯乙烯（PND- b -PS- C 12）二嵌段聚合物是通过可逆加成-断裂链转移（RAFT）聚合反应合成的，其中热响应性PND电晕嵌段的分子量保持恒定，而聚苯乙烯核心嵌段的长度却有所变化。通过动态光散射（DLS）和小角度X射线散射（SAXS）的组合来定量磷酸盐缓冲液（PBS，pH = 6.5）中胶束的电晕厚度和密度。两种疏水性模型药物苯妥英钠和尼鲁米特用于检查水溶液中药物与聚合物的相互作用。2D 1显示了二嵌段聚合物胶束电晕与两种药物之间的分子间相互作用H核Overhauser效应光谱（NOESY）。随着两种药物的二嵌段聚合物胶束电晕密度的增加，通过扩散有序NMR光谱法（DOSY）量化的药物-聚合物“结合”强度也增加了。在体外的无定形固体分散体的溶解系统的研究药物类型的函数，载药量，并且将溶液状态的组件的聚合物的通过使用一个选择性或非选择性喷雾干燥溶剂。通过将药物分子储存在电晕中，在喷雾干燥之前形成胶束可显着提高苯妥英溶解和二嵌段聚合物的过饱和度。
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