Understanding a relaxation behavior in a nanoparticle suspension for drug delivery applications
Understanding a relaxation behavior in a nanoparticle suspension for drug delivery applications
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DOI：
10.1016/j.ijpharm.2007.10.001
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发表时间：
2008-03-03
影响因子：
5.8
通讯作者：
Li, S.
中科院分区：
文献类型：
--
作者：
Deng, Z.;Xu, S.;Li, S.
纳米粒子分散体在提高难溶化合物的溶出度和口服生物利用度方面表现出了良好的效果。当我们研究药物和聚合物稳定剂的相互作用以及难于溶于水的化合物A的研磨参数时，观察到在我们的纳米颗粒分散体配方中反复发生的松弛行为。使用Nanomill(R)制备纳米粒子分散体，改变研磨参数，如时间、速度和稳定剂加入量，研究它们对松弛的影响。用光散射仪和扫描电子显微镜对球磨产物的粒度和形貌进行了研究。用X-射线粉末衍射仪(XRD)对颗粒结晶度和微晶尺寸进行了表征。结果表明，球磨后，纳米粒子不断团聚形成团簇，在最初的24 h内达到最大表观尺寸，随后团簇自发松弛，几天内解离成单个初级粒子，悬浮液稳定在接近平衡的100 nm以下水平。研磨结晶药物后得到的X射线衍射峰变宽，表明形成了无序的纳米晶。改变研磨条件和稳定剂比例会影响松弛行为，并必然导致纳米颗粒悬浮配方的工艺和性能的优化。(C)2007 Elsevier B.V.保留所有权利。
Nanoparticle dispersion has demonstrated its effectiveness in improving the dissolution rate and oral bioavailability of poorly water-soluble compounds. When we studied the interactions of drug and polymeric stabilizers and milling parameters of a poorly water-soluble compound, Compound A, the relaxation behavior that occurred repeatedly in our nanoparticle dispersion formulation was observed. Nanomill (R) was used to generate the nanoparticle dispersion, and milling parameters such as time, speed, and stabilizer loading were altered to investigate their effects on relaxation. The particle size and morphology of milled products were studied using a light-scattering particle analyzer and a scanning electron microscope (SEM). X-ray powder diffraction (XRD) was employed to characterize particle crystallinity and the crystallite size. The results indicated that, after milling, nanoparticles agglomerated constantly to form clusters and reached maximum apparent size within the first 24 h. Thereafter, the clusters relaxed spontaneously and, within a few days, dissociated into individual primary particles and the suspension were stable at sub 100-nm levels near equilibrium. Milling crystalline drug substance resulted in an XRD pattern in which the peaks were observed to broaden, suggesting formation of disordered nanocrystalline. Altering milling conditions and stabilizer ratios influences the relaxation behavior and certainly led to optimization of the process and performance of nanoparticle suspension formulations. (c) 2007 Elsevier B.V. All rights reserved.