On the Road to Development of an in Vitro Permeation Test (IVPT) Model to Compare Heat Effects on Transdermal Delivery Systems: Exploratory Studies with Nicotine and Fentanyl.
On the Road to Development of an in Vitro Permeation Test (IVPT) Model to Compare Heat Effects on Transdermal Delivery Systems: Exploratory Studies with Nicotine and Fentanyl.
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开发体外渗透测试 (IVPT) 模型以比较对透皮给药系统的热效应：尼古丁和芬太尼的探索性研究。
DOI：
10.1007/s11095-017-2189-0
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发表时间：
2017
影响因子：
3.7
通讯作者：
Stinchcomb,AudraL
中科院分区：
文献类型：
--
作者：
Shin,SooHyeon;Ghosh,Priyanka;Newman,Bryan;Hammell,DanaC;Raney,SamG;Hassan,HazemE;Stinchcomb,AudraL
目的：在温度升高的情况下，经皮给药系统（TDS）的药物释放和皮肤渗透速度可能高于正常皮肤温度。本研究的目的是利用体外透渗试验（IVPT）比较热对不同配方的基质型tds中两种模型药物尼古丁和芬太尼的透皮递送的影响。方法用猪皮对两种尼古丁类和三种芬太尼类tds进行了sivpt实验。通过加热TDS最大推荐磨损时间或短时间，研究了连续和瞬态热暴露。结果两种尼古丁tds的持续热暴露产生了不同的效果，其中一种产品表现出持久的热效应，而另一种产品则没有。两种尼古丁TDS由于持续热效应引起的jmaxenhanced ratio具有可比性，而三种芬太尼TDS之间存在显著差异（p< 0.05）。瞬时热暴露引起的jmax增强比在两种尼古丁tds中有显著差异，而在三种芬太尼tds中没有显著差异。此外，两种药物的瞬时热暴露对TDS去除后药物从皮肤库中清除的影响不同，芬太尼表现出更长的热效应。结论本探索性工作提示IVPT研究可能能够区分不同TDS在高温下经皮给药的差异。然而，IVPT热效应研究的临床意义还需通过类似研究设计的体内临床研究进一步探讨。
PurposeAt elevated temperatures, the rate of drug release and skin permeation from transdermal delivery systems (TDS) may be higher than at a normal skin temperature. The aim of this study was to compare the effect of heat on the transdermal delivery of two model drugs, nicotine and fentanyl, from matrix-type TDSs with different formulations, usingin vitropermeation tests (IVPT).MethodsIVPT experiments using pig skin were performed on two nicotine and three fentanyl TDSs. Both continuous and transient heat exposures were investigated by applying heat either for the maximum recommended TDS wear duration or for short duration.ResultsContinuous heat exposure for the two nicotine TDSs resulted in different effects, showing a prolonged heat effect for one product but not the other. The Jmaxenhancement ratio due to the continuous heat effect was comparable between the two nicotine TDS, but significantly different (p< 0.05) among the three fentanyl TDSs. The Jmaxenhancement ratios due to transient heat exposure were significantly different for the two nicotine TDSs, but not for the three fentanyl TDSs. Furthermore, the transient heat exposure affected the clearance of drug from the skin depot after TDS removal differently for two drugs, with fentanyl exhibiting a longer heat effect.ConclusionsThis exploratory work suggests that an IVPT study may be able to discriminate differences in transdermal drug delivery when different TDS are exposed to elevated temperatures. However, the clinical significance of IVPT heat effects studies should be further explored by conductingin vivoclinical studies with similar study designs.
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DOI：
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发表时间：
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