Departamento de Farmácia, Universidade Federal de Juiz de Fora (UFJF), Campus Governador Valadares, Av. Dr. Raimundo Monteiro de Rezende, 330, Centro, 35010-177 Governador Valadares, MG, Brazil.
Mater Sci Eng C Mater Biol Appl. 2013 Oct;33(7):3916-22. doi: 10.1016/j.msec.2013.05.033. Epub 2013 May 22.
Reaction of highly soluble orally active, non-peptide antihypertensive drug losartan with copper(II) leads to the spontaneous formation of a very insoluble 2:1 covalent complex, which self assembles in a hydrophobic supramolecular structure of nanometric dimensions. Thermal analysis showed that Los/Cu(II) complex presents intermediate stability in comparison with its precursors KLos and Cu(OAc)2·H2O. Isothermal titration calorimetry indicated complexation to be a stepwise process, driven by enthalpy and entropy. Zeta potential and DLS measurements showed that it is possible to control the size and charge of nanoprecipitates by adjusting the relative concentration of Los(-) and Cu(II).
高度水溶性、口服活性的非肽类抗高血压药物洛沙坦与铜（II）反应会自发形成非常不溶的 2:1 共价配合物，该配合物自组装成具有纳米级尺寸的疏水性超分子结构。热分析表明，与前体 KLOS 和 Cu(OAc)2·H2O 相比，Los/Cu(II)配合物具有中等稳定性。等温滴定量热法表明，配合作用是一个逐步过程，由焓和熵驱动。Zeta 电位和 DLS 测量表明，可以通过调节 Los(-)和 Cu(II)的相对浓度来控制纳米沉淀物的尺寸和电荷。
