Microneedle-mediated delivery of donepezil: Potential for improved treatment options in Alzheimer's disease
Microneedle-mediated delivery of donepezil: Potential for improved treatment options in Alzheimer's disease
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DOI：
10.1016/j.ejpb.2016.03.026
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发表时间：
2016-06-01
影响因子：
4.9
通讯作者：
Donnelly, Ryan F.
中科院分区：
文献类型：
--
作者：
Kearney, Mary-Carmel;Caffarel-Salvador, Ester;Donnelly, Ryan F.
透皮给药是一种有吸引力的给药途径；然而，市售的透皮产品相对较少。为了增加穿过皮肤的输送，人们广泛研究了增强皮肤渗透性的策略，其中微针显示出特别的前景。将形成水凝胶的微针插入皮肤中，在负载药物的储库溶解并且药物通过所创建的通道移动之后，微针阵列被完整地移除，然后可以容易且安全地丢弃。本研究介绍了含有阿尔茨海默病药物盐酸多奈哌齐的集成微针贴片的配方和评估。该集成贴片由形成水凝胶的微针和含有盐酸多奈哌齐的薄膜组成。介绍了由聚（乙烯基吡咯烷酮）或聚（甲基乙烯基醚共聚马来酸酐/酸）（Gantrez (R)）聚合物制备的增塑薄膜的配方和表征。此外，还研究了盐酸多奈哌齐从贴剂穿过新生猪皮肤的体外渗透情况，使用最佳贴剂配方，24小时后递送了854.71μg+/-122.71μg盐酸多奈哌齐。将贴剂施用到动物模型后，获得了 51.8 +/- 17.6 ng/mL 的血浆浓度，证明了该盐酸多奈哌齐递送平台的成功。 (C) 2016 年作者。由 Elsevier B.V. 出版
Transdermal drug delivery is an attractive route of drug administration; however, there are relatively few marketed transdermal products. To increase delivery across the skin, strategies to enhance skin permeability are widely investigated, with microneedles demonstrating particular promise. Hydrogel-forming microneedles are inserted into the skin, and following dissolution of a drug loaded reservoir and movement of the drug through the created channels, the microneedle array is removed intact, and can then be readily and safely discarded. This study presents the formulation and evaluation of an integrated micro needle patch containing the Alzheimer's drug, donepezil hydrochloride. The integrated patch consisted of hydrogel-forming microneedles in combination with a donepezil hydrochloride containing film. Formulation and characterisation of plasticised films, prepared from poly(vinylpyrrolidone) or poly (methyl vinyl ether co-maleic anhydride/acid) (Gantrez (R)) polymers, is presented. Furthermore, in vitro permeation of donepezil hydrochloride across neonatal porcine skin from the patches was investigated, with 854.71 mu g +/- 122.71 mu g donepezil hydrochloride delivered after 24 h, using the optimum patch formulation. Following administration of the patch to an animal model, plasma concentrations of 51.8 +/- 17.6 ng/mL were obtained, demonstrating the success of this delivery platform for donepezil hydrochloride. (C) 2016 The Authors. Published by Elsevier B.V.