Assessment of Drug Delivery Kinetics to Epidermal Targets In Vivo.
Assessment of Drug Delivery Kinetics to Epidermal Targets In Vivo.
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DOI：
10.1208/s12248-021-00571-3
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发表时间：
2021-03-29
期刊：
影响因子：
--
通讯作者：
Guy RH
中科院分区：
文献类型：
--
作者：
Hoppel M;Tabosa MAM;Bunge AL;Delgado-Charro MB;Guy RH
事实证明，量化从配方到可存活皮肤的“药物输入”具有挑战性，因为局部应用药物的表皮和真皮目标很难（如果不是不可能的话）在体内获得。用一种简单实用的实验方法定义可存活皮肤的药物输入功能，将使皮肤药代动力学的关键组成部分得以表征。据推测，通过胶带剥离测量药物进入角质层（SC）和从角质层（SC）清除的情况，可以估计局部药物进入活组织的输入功能。这项研究的目的是通过测定尼古丁和利多卡因的输入量来测试这一想法，随后将商业化的透皮贴片应用于健康的人类志愿者。这些输送系统的已知输入率被用来验证和评估胶带剥离方案的结果。体内贴片剥离的药物输入率与贴片声称的递送率很好地吻合。然后，实验方法被用于确定从市场上销售的乳膏中输入利多卡因，这是一种典型的外用产品，其药物吸收量尚未得到很好的表征。发现从药膏中释放的利多卡因明显高于从贴片中释放的利多卡因。在体外常规扩散细胞中，以猪腹部皮肤为实验材料，定性和定量地证实了药物和制剂在体内的不同输入率。在线版本包含补充材料，可在10.1208/s12248-021-00571-3获得。
It has proven challenging to quantify ‘drug input’ from a formulation to the viable skin because the epidermal and dermal targets of topically applied drugs are difficult, if not impossible, to access in vivo. Defining the drug input function to the viable skin with a straightforward and practical experimental approach would enable a key component of dermal pharmacokinetics to be characterised. It has been hypothesised that measuring drug uptake into and clearance from the stratum corneum (SC) by tape-stripping allows estimation of a topical drug’s input function into the viable tissue. This study aimed to test this idea by determining the input of nicotine and lidocaine into the viable skin, following the application of commercialised transdermal patches to healthy human volunteers. The known input rates of these delivery systems were used to validate and assess the results from the tape-stripping protocol. The drug input rates from in vivo tape-stripping agreed well with the claimed delivery rates of the patches. The experimental approach was then used to determine the input of lidocaine from a marketed cream, a typical topical product for which the amount of drug absorbed has not been well-characterised. A significantly higher delivery of lidocaine from the cream than from the patch was found. The different input rates between drugs and formulations in vivo were confirmed qualitatively and quantitatively in vitro in conventional diffusion cells using dermatomed abdominal pig skin. The online version contains supplementary material available at 10.1208/s12248-021-00571-3.
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影响因子：
5.8
作者：
Cordery SF;Pensado A;Chiu WS;Shehab MZ;Bunge AL;Delgado-Charro MB;Guy RH
通讯作者：
Guy RH
影响因子：
5.8
作者：
Mitragotri, Samir;Anissimov, Yuri G.;Roberts, Michael S.
通讯作者：
Roberts, Michael S.
影响因子：
3.4
作者：
HO, H;CHIEN, YW
通讯作者：
CHIEN, YW
影响因子：
5.8
作者：
LEE, PH;SU, MH;HIGUCHI, WI
通讯作者：
HIGUCHI, WI
影响因子：
3.7
作者：
N'Dri-Stempfer, Berthe;Navidi, William C.;Bunge, Annette L.
通讯作者：
Bunge, Annette L.