当前位置: X-MOL 学术Starch › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Interaction of Tretinoin and Nimesulide with Amylose Matrices
Starch ( IF 2.3 ) Pub Date : 2020-07-01 , DOI: 10.1002/star.202000054
Anna Marinopoulou 1 , Dimitrios Christofilos 2 , John Arvanitidis 3 , Stylianos N. Raphaelides 1
Affiliation  

Systems of amylose with nimesulide or tretinoin are prepared and characterized in order to evaluate their in vitro release behavior. X‐ray diffraction (XRD) data of the amylose systems containing drug molecules reveal patterns characteristic of the V‐type of complexed amylose. Nevertheless, they cannot be unequivocally assigned to complexed amylose since both drugs exhibit XRD reflections at similar 2‐theta angles. Raman scattering and differential scanning calorimetry thermal analysis provide evidence suggesting that tretinoin is more likely to form molecular inclusion complexes than nimesulide. The drug–amylose interaction is also assessed by means of optical microscopy, confocal laser scanning microscopy, and scanning electron microscopy. The results reveal that the drug molecules are effectively entrapped in the amylose matrix, probably inside or between the amylose helices. Acidic and enzymatic tests allow the quantification of the drug molecules released from the matrix of the amylose systems with tretinoin or nimesulide. In the simulated intestinal fluid, the drug release of the samples reached up to ≈52% for tretinoin and ≈39% for nimesulide systems. Overall, the results show that the molecular interaction of amylose, with tretinoin appears to be more promising for efficient complexation than with nimesulide.

中文翻译:

维甲酸和尼美舒利与直链淀粉基质的相互作用

制备并表征了具有尼美舒利或维甲酸的直链淀粉体系,以评估其体外释放行为。含有药物分子的直链淀粉系统的X射线衍射(XRD)数据揭示了复合直链淀粉V型的特征模式。然而,由于两种药物在相似的2θ角均表现出XRD反射,因此不能明确地将它们分配给复杂的直链淀粉。拉曼散射和差示扫描量热法热分析提供了证据,表明维甲酸比尼美舒利更可能形成分子包合物。还通过光学显微镜,共聚焦激光扫描显微镜和扫描电子显微镜评估了药物-直链淀粉的相互作用。结果表明,药物分子被有效地截留在直链淀粉基质中,可能在直链螺旋内部或之间。酸性和酶促测试可以定量检测使用维甲酸或尼美舒利从直链淀粉系统基质释放的药物分子。在模拟的肠液中,维甲酸的样品释放量高达≈52%,尼美舒利系统的释放率高达≈39%。总的来说,结果表明直链淀粉与维甲酸的分子相互作用似乎比尼美舒利更有效地络合。
更新日期:2020-07-01
down
wechat
bug