Characterisation of Drug Delivery Efficacy Using Microstructure-Assisted Application of a Range of APIs.
Characterisation of Drug Delivery Efficacy Using Microstructure-Assisted Application of a Range of APIs.
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DOI：
10.3390/pharmaceutics12121213
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发表时间：
2020-12-15
期刊：
影响因子：
5.4
通讯作者：
Graz M
中科院分区：
文献类型：
--
作者：
Rahbari R;Ichim I;Bamsey R;Burridge J;Guy OJ;Bolodeoku J;Graz M
基于聚合物的固体微结构（MSts）具有显著增加可通过皮肤施用的药物的量和范围的潜力。MSt阵列被用于证明其绕过皮肤屏障并通过以微创方式创建穿过角质层的微通道来增强渗透性的能力。本研究的目的是证明MSts的能力，以超过目前的界限，透皮给药的化合物具有不同的分子量，分配系数，酸解离常数，熔点和水溶性。已经研究了一系列选定分子（包括乙酰水杨酸（阿司匹林）、加兰他敏、盐酸司来吉兰（Sel-HCl）、胰岛素、咖啡因、氢化可的松（HC）、氢化可的松21-半琥珀酸钠盐（HC-HS）和牛血清白蛋白（BSA））在有和没有MSt戳和贴片应用的离体猪皮中的体外渗透。使用Franz扩散池在24小时内监测分子的渗透。MSts显着增加渗透的所有选定的分子高达40倍，相比，局部应用的分子没有MSts。观察到咖啡因的渗透增加最大，渗透增加70 ± 8%，观察到HC的渗透增加最小，渗透增加2.4 ± 1.3%。获得的最高通量为BSA（8133 ± 1365 μg/cm 2/h），观察到的最低通量为HC（11 ± 4 μg/cm 2/h）。24 h后，BSA和HC的渗透量最大（16，275 ± 3078 μg），最小（73 ± 47 μg）。MSt处理的皮肤表现出大大增加的渗透。分子参数（大小，酸解离常数，分配系数和溶解度）-传统的障碍与被动扩散通过完整的皮肤-克服使用MSt皮肤治疗。
Polymer-based solid microstructures (MSts) have the potential to significantly increase the quantity and range of drugs that can be administered across the skin. MSt arrays are used to demonstrate their capacity to bypass the skin barrier and enhance permeability by creating microchannels through the stratum corneum, in a minimally invasive manner. This study is designed to demonstrate the ability of MSts to exceed the current boundaries for transdermal delivery of compounds with different molecular weights, partition coefficients, acid dissociation constants, melting points, and water solubilities. In vitro permeation of a range of selected molecules, including acetyl salicylic acid (aspirin), galantamine, selegiline hydrochloride (Sel-HCl), insulin, caffeine, hydrocortisone (HC), hydrocortisone 21-hemisuccinate sodium salt (HC-HS) and bovine serum albumin (BSA) has been studied across excised porcine skin with and without poke and patch application of MSts. Permeation of the molecules was monitored using Franz diffusion cells over 24 h. MSts significantly increased the permeation of all selected molecules up to 40 times, compared to topical applications of the molecules without MSts. The greatest increase in permeation was observed for caffeine with 70 ± 8% permeation and the lowest enhancement was observed for HC with a 2.4 ± 1.3% increase in permeation. The highest obtained flux was BSA (8133 ± 1365 μg/cm2/h) and the lowest flux observed for HC (11 ± 4 μg/cm2/h). BSA and HC also showed the highest (16,275 ± 3078 μg) and the lowest (73 ± 47 μg) permeation amount after 24 h respectively. MSt-treated skin exhibits greatly increased permeation. The molecule parameters (size, acid dissociation constant, partition coefficient and solubility)—traditional hurdles associated with passive diffusion through intact skin—are overcome using MSt skin treatment.
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影响因子：
5.4
作者：
Alkilani AZ;McCrudden MT;Donnelly RF
通讯作者：
Donnelly RF
影响因子：
3.2
作者：
Bare, AC;McAnaw, MB;Seal, LA
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影响因子：
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作者：
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作者：
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影响因子：
10.8
作者：
Courtenay, Aaron J.;McAlister, Emma;Donnelly, Ryan F.
通讯作者：
Donnelly, Ryan F.