Journal of drugs in dermatology : JDD · 2021
Development of a Tape-Stripping Liquid Chromatography-Mass Spectrometry Method for Evaluating Skin Deposition of Topical Tazarotene.
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Draelos Zoe D, Draelos Matthew M
Аннотация
BACKGROUND: Standard in vitro and ex vivo techniques for evaluating topical drug penetration utilize skin that is physiologically unlike living skin and cannot assess intra-dermal drug deposition. We combined tape stripping with liquid chromatography-heated electrospray ionization-mass spectrometry (LC-ESI-MS) to assess in vivo deposition of tazarotene after application of 0.1% cream and 0.045% lotion formulations.
METHODS: Ten healthy adult female participants had ~0.1 g of tazarotene lotion and cream applied to two sites each on opposite forearms. After 3 and 6 hours, 21 tape strips were used to sample progressively deeper skin layers. LC-ESI-MS was used to determine percent recovery of the applied tazarotene dose and the concentration of tazarotene recovered from even-numbered tape strips.
RESULTS: At both sampling times, percent recovery was slightly higher with tazarotene 0.045% lotion versus 0.1% cream, though tazarotene concentrations were approximately 2-fold higher for cream than lotion at both superficial and deep skin layers. Absolute differences in tazarotene concentrations between 0.1% cream and 0.045% lotion decreased in progressively deeper skin layers, from 0.8 μg/mL at tape strip 2 to 0.09 μg/mL at tape strip 20 (6 hours post-application).
CONCLUSIONS: Tape stripping plus LC-ESI-MS—a consistent, accurate, and non-invasive method for assessing drug delivery into layers of living skin—can be used to assess in vivo deposition of topical formulations. Results from this study, when combined with clinical data, suggest that small tazarotene-deposition differences between lotion and cream in deeper skin layers are not clinically relevant; however, lower-dose 0.045% lotion may minimize tazarotene skin exposure versus 0.1% cream, potentially resulting in a more favorable tolerability profile. J Drugs Dermatol. 2021;20(10):1105-1111. doi:10.36849/JDD.6211.
METHODS: Ten healthy adult female participants had ~0.1 g of tazarotene lotion and cream applied to two sites each on opposite forearms. After 3 and 6 hours, 21 tape strips were used to sample progressively deeper skin layers. LC-ESI-MS was used to determine percent recovery of the applied tazarotene dose and the concentration of tazarotene recovered from even-numbered tape strips.
RESULTS: At both sampling times, percent recovery was slightly higher with tazarotene 0.045% lotion versus 0.1% cream, though tazarotene concentrations were approximately 2-fold higher for cream than lotion at both superficial and deep skin layers. Absolute differences in tazarotene concentrations between 0.1% cream and 0.045% lotion decreased in progressively deeper skin layers, from 0.8 μg/mL at tape strip 2 to 0.09 μg/mL at tape strip 20 (6 hours post-application).
CONCLUSIONS: Tape stripping plus LC-ESI-MS—a consistent, accurate, and non-invasive method for assessing drug delivery into layers of living skin—can be used to assess in vivo deposition of topical formulations. Results from this study, when combined with clinical data, suggest that small tazarotene-deposition differences between lotion and cream in deeper skin layers are not clinically relevant; however, lower-dose 0.045% lotion may minimize tazarotene skin exposure versus 0.1% cream, potentially resulting in a more favorable tolerability profile. J Drugs Dermatol. 2021;20(10):1105-1111. doi:10.36849/JDD.6211.