Evaluation of drug interactions with nanofibrillar cellulose
Evaluation of drug interactions with nanofibrillar cellulose
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DOI：
10.1016/j.ejpb.2013.05.015
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发表时间：
2013-11-01
影响因子：
4.9
通讯作者：
Laaksonen, Timo
中科院分区：
文献类型：
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作者：
Kolakovic, Ruzica;Peltonen, Leena;Laaksonen, Timo
纳米原纤纤维素（NFC）（也称为纤维素纳米纤维、纳米纤维素、微原纤化或纳米原纤化纤维素）最近在各个研究领域受到广泛关注，并且它也被研究作为药物剂型配方中的赋形剂。在这里，我们评估了 NFC 与不同结构特征（尺寸、电荷等）的模型药物之间的相互作用。这一系列的渗透研究用于评估溶液中的药物通过多孔干燥 NFC 薄膜扩散的能力。使用孵育方法来确定所选模型药物与 NFC 的结合能力，并使用等温滴定量热法 (ITC) 来研究结合过程的热力学。携带双纤维素结合域的基因工程融合蛋白被用作阳性对照，因为其对 NFC 的亲和力和结合能力已被报道。渗透研究揭示了模型药物通过 NFC 薄膜的尺寸依赖性扩散速率。结合和 ITC 研究的结果表明，所研究的药物与 NFC 材料结合，并表明结合力和静电力的 pH 依赖性是主要机制。 (C) 2013 Elsevier B.V. 保留所有权利。
Nanofibrillar cellulose (NFC) (also referred to as cellulose nanofibers, nanocellulose, microfibrillated, or nanofibrillated cellulose) has recently gotten wide attention in various research areas and it has also been studied as excipient in formulation of the pharmaceutical dosage forms. Here, we have evaluated the interactions between NFC and the model drugs of different structural characteristics (size, charge, etc.). The series of permeation studies were utilized to evaluate the ability of the drugs in solution to diffuse through the thin, porous, dry NFC films. An incubation method was used to determine capacity of binding of chosen model drugs to NFC as well as isothermal titration calorimetry (ITC) to study thermodynamics of the binding process. A genetically engineered fusion protein carrying double cellulose binding domain was used as a positive control since its affinity and capacity of binding for NFC have already been reported. The permeation studies revealed the size dependent diffusion rate of the model drugs through the NFC films. The results of both binding and ITC studies showed that the studied drugs bind to the NFC material and indicated the pH dependence of the binding and electrostatic forces as the main mechanism. (C) 2013 Elsevier B.V. All rights reserved.