聚合物与enzalutamide Nanodroplet的相互作用 - 对液滴特性和诱导时间的影响
由分散在聚合物基质中的药物组成的无定形固体分散体（ASD）越来越多地用于改进体内口服水溶性药物不良的性能。聚合物是一个关键的成分，扮演多个角色，包括促进ASD的药物释放，并延迟溶解后产生的过饱和溶液的结晶。
某些ASD制剂溶解以产生无定形药物富含药物的纳米光。聚合物与这些纳米光的相互作用知之甚少，但被认为对于抑制这些系统的结晶很重要。在这项研究中，通过确定成核诱导时间评估了离子聚合物对含有不同量的无定形纳米光的过饱和溶液的结晶动力学的影响。还确定了与药物纳米光相关的聚合物的量。在比较两种聚合物时，乙酸羟基甲基纤维素琥珀酸酯（HPMCAS） 和Eudragit E Po, it was found that the crystallization tendency and physical properties of the drug nanodroplets varied in the presence of these two polymers. Both polymers distributed between the aqueous phase and the drug-rich nanodroplets. A greater amount of Eudragit E PO was associated with the drug-rich nanodroplets.
Despite this, Eudragit E PO was a less-effective crystallization inhibitor than HPMCAS in systems containing nanodroplets. In conclusion, in supersaturated solutions containing amorphous nanodroplets, the extent of association of a polymer with the drug nanodroplet does not solely predict crystallization inhibition.
文章信息：Venecia R. Wilson，Naila A. Mugheirbi，Laura I. Mosquera-Giraldo，Alexandru Deac，Dana E. Moseson，Daniel T. Smith，Diana C. Novo，Carlos H.埃德加（Edgar）和林恩·泰勒（Lynne S.分子药物尽快。DOI: 10.1021 / acs.molpharmaceut.0c00833