Coating solid dispersions on microneedles via a molten dip-coating method: development and in vitro evaluation for transdermal delivery of a water-insoluble drug.
Coating solid dispersions on microneedles via a molten dip-coating method: development and in vitro evaluation for transdermal delivery of a water-insoluble drug.
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DOI：
10.1002/jps.24159
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发表时间：
2014-11
影响因子：
3.8
通讯作者：
Gill, Harvinder S.
中科院分区：
文献类型：
--
作者：
Ma, Yunzhe;Gill, Harvinder S.
这项研究首次证明了将固体分散体包裹在微针上作为一种通过皮肤传递水不溶性药物的手段的能力。以聚乙二醇为亲水基质，以利多卡因碱为模型疏水药物制备固体分散体。首先，对不同质量分数的聚乙二醇利多卡因混合物进行了热表征和粘度测量。结果表明，利多卡因可在~130℃温度下保持稳定，且随着利多卡因质量分数的降低，聚乙二醇利多卡因熔体的粘度增大。差示扫描量热分析表明，当利多卡因质量分数小于或等于50%时，利多卡因在聚乙二醇利多卡因混合物中分散良好。在微针表面获得了均匀的涂层。猪皮肤体外溶出度研究表明，涂有聚乙二醇利多卡因分散体的微针在3分钟内的利多卡因释放量显著高于商业利多卡因-普利卡因乳膏0.15 g EMLA®外用1小时。总之，我们在这里介绍的熔融包衣工艺为将水不溶性药物包衣在微针上以进行经皮给药提供了一种实用的方法。
This study demonstrates for the first time the ability to coat solid dispersions on microneedles as a means to deliver water-insoluble drugs through the skin. Polyethylene glycol (PEG) was selected as the hydrophilic matrix, and lidocaine base was selected as the model hydrophobic drug to create the solid dispersion. First, thermal characterization and viscosity measurements of the PEG-lidocaine mixture at different mass fractions were performed. The results show that lidocaine can remain stable at temperatures up to ~130 °C, and that viscosity of the PEG-lidocaine molten solution increases as the mass fraction of lidocaine decreases. Differential scanning calorimetry demonstrated that at lidocaine mass fraction less than or equal to 50%, lidocaine is well dispersed in the PEG-lidocaine mixture. Uniform coatings were obtained on microneedle surfaces. In vitro dissolution studies in porcine skin showed that microneedles coated with PEG-lidocaine dispersions resulted in significantly higher delivery of lidocaine in just 3 min compared to 1 h topical application of 0.15 g EMLA®, a commercial lidocaine-prilocaine cream. In conclusion, the molten coating process we introduce here offers a practical approach to coat water-insoluble drugs on microneedles for transdermal delivery.
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