Reduction of focal sweating by lipid nanoparticle-delivered myricetin

Choongjin Ban; Joon Bum Park; Sora Cho; Hye Rin Kim; Yong Joon Kim; Young Jin Choi; Woo Jae Chung; Dae Hyuk Kweon

doi:10.1038/s41598-020-69985-x

Reduction of focal sweating by lipid nanoparticle-delivered myricetin

Choongjin Ban, Joon Bum Park, Sora Cho, Hye Rin Kim, Yong Joon Kim, Young Jin Choi, Woo Jae Chung, Dae Hyuk Kweon

Department of Environmental Horticulture

Research output: Contribution to journal › Article › peer-review

14 Scopus citations

Abstract

Myricetin—a flavonoid capable of inhibiting the SNARE complex formation in neurons—reduces focal sweating after skin-application when delivers as encapsulated in lipid nanoparticles (M-LNPs). The stability of M-LNP enables efficient delivery of myricetin to sudomotor nerves located underneath sweat glands through transappendageal pathways while free myricetin just remained on the skin. Furthermore, release of myricetin from M-LNP is accelerated through lipase-/esterase-induced lipolysis in the skin-appendages, enabling uptake of myricetin by the surrounding cells. The amount of sweat is reduced by 55% after application of M-LNP (0.8 mg kg⁻¹) on the mouse footpad. This is comparable to that of subcutaneously injected anticholinergic agents [0.25 mg kg⁻¹ glycopyrrolate; 0.8 U kg⁻¹ botulinum neurotoxin-A-type (BoNT/A)]. M-LNP neither shows a distal effect after skin-application nor induced cellular/ocular toxicity. In conclusion, M-LNP is an efficient skin-applicable antiperspirant. SNARE-inhibitory small molecules with suitable delivery systems have the potential to replace many BoNT/A interventions for which self-applications are preferred.

Original language	English
Article number	13132
Journal	Scientific Reports
Volume	10
Issue number	1
DOIs	https://doi.org/10.1038/s41598-020-69985-x
State	Published - 1 Dec 2020

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title = "Reduction of focal sweating by lipid nanoparticle-delivered myricetin",

abstract = "Myricetin—a flavonoid capable of inhibiting the SNARE complex formation in neurons—reduces focal sweating after skin-application when delivers as encapsulated in lipid nanoparticles (M-LNPs). The stability of M-LNP enables efficient delivery of myricetin to sudomotor nerves located underneath sweat glands through transappendageal pathways while free myricetin just remained on the skin. Furthermore, release of myricetin from M-LNP is accelerated through lipase-/esterase-induced lipolysis in the skin-appendages, enabling uptake of myricetin by the surrounding cells. The amount of sweat is reduced by 55% after application of M-LNP (0.8 mg kg−1) on the mouse footpad. This is comparable to that of subcutaneously injected anticholinergic agents [0.25 mg kg−1 glycopyrrolate; 0.8 U kg−1 botulinum neurotoxin-A-type (BoNT/A)]. M-LNP neither shows a distal effect after skin-application nor induced cellular/ocular toxicity. In conclusion, M-LNP is an efficient skin-applicable antiperspirant. SNARE-inhibitory small molecules with suitable delivery systems have the potential to replace many BoNT/A interventions for which self-applications are preferred.",

author = "Choongjin Ban and Park, {Joon Bum} and Sora Cho and Kim, {Hye Rin} and Kim, {Yong Joon} and Choi, {Young Jin} and Chung, {Woo Jae} and Kweon, {Dae Hyuk}",

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AU - Ban, Choongjin

AU - Park, Joon Bum

AU - Cho, Sora

AU - Kim, Hye Rin

AU - Kim, Yong Joon

AU - Choi, Young Jin

AU - Chung, Woo Jae

AU - Kweon, Dae Hyuk

PY - 2020/12/1

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N2 - Myricetin—a flavonoid capable of inhibiting the SNARE complex formation in neurons—reduces focal sweating after skin-application when delivers as encapsulated in lipid nanoparticles (M-LNPs). The stability of M-LNP enables efficient delivery of myricetin to sudomotor nerves located underneath sweat glands through transappendageal pathways while free myricetin just remained on the skin. Furthermore, release of myricetin from M-LNP is accelerated through lipase-/esterase-induced lipolysis in the skin-appendages, enabling uptake of myricetin by the surrounding cells. The amount of sweat is reduced by 55% after application of M-LNP (0.8 mg kg−1) on the mouse footpad. This is comparable to that of subcutaneously injected anticholinergic agents [0.25 mg kg−1 glycopyrrolate; 0.8 U kg−1 botulinum neurotoxin-A-type (BoNT/A)]. M-LNP neither shows a distal effect after skin-application nor induced cellular/ocular toxicity. In conclusion, M-LNP is an efficient skin-applicable antiperspirant. SNARE-inhibitory small molecules with suitable delivery systems have the potential to replace many BoNT/A interventions for which self-applications are preferred.

AB - Myricetin—a flavonoid capable of inhibiting the SNARE complex formation in neurons—reduces focal sweating after skin-application when delivers as encapsulated in lipid nanoparticles (M-LNPs). The stability of M-LNP enables efficient delivery of myricetin to sudomotor nerves located underneath sweat glands through transappendageal pathways while free myricetin just remained on the skin. Furthermore, release of myricetin from M-LNP is accelerated through lipase-/esterase-induced lipolysis in the skin-appendages, enabling uptake of myricetin by the surrounding cells. The amount of sweat is reduced by 55% after application of M-LNP (0.8 mg kg−1) on the mouse footpad. This is comparable to that of subcutaneously injected anticholinergic agents [0.25 mg kg−1 glycopyrrolate; 0.8 U kg−1 botulinum neurotoxin-A-type (BoNT/A)]. M-LNP neither shows a distal effect after skin-application nor induced cellular/ocular toxicity. In conclusion, M-LNP is an efficient skin-applicable antiperspirant. SNARE-inhibitory small molecules with suitable delivery systems have the potential to replace many BoNT/A interventions for which self-applications are preferred.

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Reduction of focal sweating by lipid nanoparticle-delivered myricetin

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