Topical bioavailability of diclofenac from locally-acting, dermatological formulations.
Topical bioavailability of diclofenac from locally-acting, dermatological formulations.
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DOI：
10.1016/j.ijpharm.2017.06.063
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发表时间：
2017-08-30
影响因子：
5.8
通讯作者：
Guy RH
中科院分区：
文献类型：
--
作者：
Cordery SF;Pensado A;Chiu WS;Shehab MZ;Bunge AL;Delgado-Charro MB;Guy RH
评估局部应用药物的生物利用度是一个具有挑战性的目标。一些不同但可能互补的技术正在评估之中。本研究的目的是评价体外皮肤渗透和体内角质层胶带剥离，作为测量三种获批和市售产品（两种凝胶和一种溶液）的局部双氯芬酸生物利用度的工具。使用人类志愿者角质层的药物摄取及其随后的清除率来估计双氯芬酸进入活性皮肤层的输入速率。将该通量与在常规扩散池中穿过切除的猪皮肤测量的通量进行比较。两种技术均清楚地证明了（a）溶液中药物递送的优越性，以及（B）两种凝胶的性能相似。有定性和，重要的是，定量协议之间的药物流入和超出可行的皮肤在体外和体内测量。因此，有证据支持评估局部药物生物利用度的方法之间的体内-体外相关性。角质层胶带剥离技术的潜在价值，以量化药物输送到（表皮）真皮和皮下组织下的屏障被证明。
Assessment of the bioavailability of topically applied drugs designed to act within or beneath the skin is a challenging objective. A number of different, but potentially complementary, techniques are under evaluation. The objective of this work was to evaluate in vitro skin penetration and stratum corneum tape-stripping in vivo as tools with which to measure topical diclofenac bioavailability from three approved and commercialized products (two gels and one solution). Drug uptake into, and its subsequent clearance from, the stratum corneum of human volunteers was used to estimate the input rate of diclofenac into the viable skin layers. This flux was compared to that measured across excised porcine skin in conventional diffusion cells. Both techniques clearly demonstrated (a) the superiority in terms of drug delivery from the solution, and (b) that the two gels performed similarly. There was qualitative and, importantly, quantitative agreement between the in vitro and in vivo measurements of drug flux into and beyond the viable skin. Evidence is therefore presented to support an in vivo — in vitro correlation between methods to assess topical drug bioavailability. The potential value of the stratum corneum tape-stripping technique to quantify drug delivery into (epi)dermal and subcutaneous tissue beneath the barrier is demonstrated.
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影响因子：
3.4
作者：
Kalia, YN;Pirot, F;Guy, RH
通讯作者：
Guy, RH
影响因子：
3.8
作者：
MAITANI, Y;COUTELEGROS, A;NAGAI, T
通讯作者：
NAGAI, T
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.
影响因子：
3.7
作者：
Herkenne, Christophe;Alberti, Ingo;Naik, Aarti;Kalia, Yogeshvar N.;Mathy, Franois-Xavier;Preat, Veronique;Guy, Richard H.
通讯作者：
Guy, Richard H.
影响因子：
4.5
作者：
Chang, Rong-Kun;Raw, Andre;Yu, Lawrence
通讯作者：
Yu, Lawrence