A facile system to evaluate in vitro drug release from dissolving microneedle arrays.
A facile system to evaluate in vitro drug release from dissolving microneedle arrays.
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DOI：
10.1016/j.ijpharm.2015.11.038
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发表时间：
2016-01-30
影响因子：
5.8
通讯作者：
Donnelly RF
中科院分区：
文献类型：
--
作者：
Larrañeta E;Stewart S;Fallows SJ;Birkhäuer LL;McCrudden MT;Woolfson AD;Donnelly RF
在体外评估溶解（?）微针（MN）阵列机械强度和随后的药物释放概况时，使用生物组织存在一些基本困难，部分原因是所使用的生物组织的固有可变性。因此，这些生物材料不适合在工业配方开发或质量控制（QC）测试中常规使用。在目前的工作中，提出了一种使用Parafilm®（PF）来测试溶解MN阵列药物渗透性能的简便系统。将包含196根针（针高600 μm）的溶解MN阵列插入到单层PF中，形成一个密封的“袋”，包括内部的阵列。将得到的体系置于溶解浴中，并评估模型分子的释放。使用这种新装置测试了不同的MN配方，在6小时后释放40至180 μg的产物。与文献中描述的传统透皮贴剂的典型性能测试相比，所提出的系统是一种更现实的MN测试方法。此外，在密封“袋”中测试了PF膜的使用，并使用Franz Cell方法获得了可比的释放曲线。显微镜用于确定不同MN阵列在PF层中的插入。所提出的系统似乎是一个很好的替代使用弗朗茨细胞，以比较不同的锰配方。考虑到工业对MN技术的兴趣日益增加，所提议的系统有潜力作为质量控制目的的标准化药物/活性剂释放测试。
The use of biological tissues in the in vitro assessments of dissolving (?) microneedle (MN) array mechanical strength and subsequent drug release profiles presents some fundamental difficulties, in part due to inherent variability of the biological tissues employed. As a result, these biological materials are not appropriate for routine used in industrial formulation development or quality control (QC) tests. In the present work a facile system using Parafilm M® (PF) to test drug permeation performance using dissolving MN arrays is proposed. Dissolving MN arrays containing 196 needles (600 μm needle height) were inserted into a single layer of PF and a hermetic “pouch” was created including the array inside. The resulting system was placed in a dissolution bath and the release of model molecules was evaluated. Different MN formulations were tested using this novel setup, releasing between 40 and 180 μg of their cargos after 6 h. The proposed system is a more realistic approach for MN testing than the typical performance test described in the literature for conventional transdermal patches. Additionally, the use of PF membrane was tested either in the hermetic “pouch” and using Franz Cell methodology yielding comparable release curves. Microscopy was used in order to ascertain the insertion of the different MN arrays in the PF layer. The proposed system appears to be a good alternative to the use of Franz cells in order to compare different MN formulations. Given the increasing industrial interest in MN technology, the proposed system has potential as a standardised drug/active agent release test for quality control purposes.