Preparation and characterization of hydroxypropyl methyl cellulose films containing stable BCS Class II drug nanoparticles for pharmaceutical applications
Preparation and characterization of hydroxypropyl methyl cellulose films containing stable BCS Class II drug nanoparticles for pharmaceutical applications
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DOI：
10.1016/j.ijpharm.2011.12.001
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发表时间：
2012-02-28
影响因子：
5.8
通讯作者：
Dave, Rajesh N.
中科院分区：
文献类型：
--
作者：
Sievens-Figueroa, Lucas;Bhakay, Anagha;Dave, Rajesh N.
一个简单的过程中，将稳定的纳米粒子到可食用的聚合物薄膜的设计和可行性证明与提高水溶性差的药物的溶解速率的目标。通过与含有甘油的低分子量羟丙基甲基纤维素（HPMC E15 LV）溶液混合，然后通过膜浇铸和干燥，将由湿搅拌介质研磨（WSMM）产生的纳米悬浮液转化为含有药物纳米颗粒的聚合物膜。研究了三种不同的BCS II类药物，萘普生（NPX）、非诺贝特（FNB）和灰黄霉素（GF）。并考察了药物分子对涂膜性能的影响。根据X射线衍射（XRD）和拉曼光谱，结果表明所采用的膜处理方法对药物结晶度没有影响。通过扫描电镜和近红外化学成像分析观察了原料药在膜中聚集行为的差异。与其他药物相比，NPX表现出最强的聚集。聚集对药物在膜中的含量均匀性有直接影响。膜的机械性能也受到药物-聚合物相互作用的影响。由于与聚合物的强氢键，NPX表现出约200%的杨氏模量（YM）的增加，以及其他机械性能，相比于GF膜。FNB膜中表面活性剂/聚合物和药物/聚合物相互作用之间的协同效应导致YM比GF膜增加600%以上。由于膜的大表面积和较小的药物粒径，药物溶出速率的增强也被证明。(C)2011 Elsevier B. V.保留所有权利。
The design and feasibility of a simple process of incorporating stable nanoparticles into edible polymer films is demonstrated with the goal of enhancing the dissolution rate of poorly water soluble drugs. Nanosuspensions produced from wet stirred media milling (WSMM) were transformed into polymer films containing drug nanoparticles by mixing with a low molecular weight hydroxylpropyl methyl cellulose (HPMC E15LV) solution containing glycerin followed by film casting and drying. Three different BCS Class II drugs, naproxen (NPX), fenofibrate (FNB) and griseofulvin (GF) were studied. The influence of the drug molecule on the film properties was also investigated. It was shown that film processing methodology employed has no effect on the drug crystallinity according to X-ray diffraction (XRD) and Raman spectroscopy. Differences in aggregation behavior of APIs in films were observed through SEM and NIR chemical imaging analysis. NPX exhibited the strongest aggregation compared to the other drugs. The aggregation had a direct effect on drug content uniformity in the film. Mechanical properties of the film were also affected depending on the drug-polymer interaction. Due to strong hydrogen bonding with the polymer, NPX exhibited an increase in Young's Modulus (YM) of approximately 200%, among other mechanical properties, compared to GF films. A synergistic effect between surfactant/polymer and drug/polymer interactions in the FNB film resulted in an increase of more than 600% in YM compared to the GF film. The enhancement in drug dissolution rate of films due to the large surface area and smaller drug particle size was also demonstrated. (C) 2011 Elsevier B.V. All rights reserved.