Enhanced Transdermal Delivery by Combined Application of Dissolving Microneedle Patch on Serum-Treated Skin

Suyong Kim, Manita Dangol, Geonwoo Kang, Shayan F. Lahiji, Huisuk Yang, Mingyu Jang, Yonghao Ma, Chengguo Li, Sang Gon Lee, Chang Hyun Kim, Young Wook Choi, So Jeong Kim, Ja Hyun Ryu, Ji Hwoon Baek, Jaesuk Koh, Hyungil Jung

Research output: Contribution to journalArticle

13 Citations (Scopus)

Abstract

Dissolving microneedle (DMN), a transdermal drug delivery system in which drugs are encapsulated in a biodegradable polymeric microstructure, is designed to dissolve after skin penetration and release the encapsulated drugs into the body. However, because of limited loading capacity of drugs within microsized structures, only a small dosage can be delivered, which is often insufficient for patients. We propose a novel DMN application that combines topical and DMN application simultaneously to improve skin permeation efficiency. Drugs in pretreated topical formulation and encapsulated drugs in DMN patch are delivered into the skin through microchannels created by DMN application, thus greatly increasing the delivered dose. We used 4-n-butylresorcinol to treat human hyperpigmentation and found that sequential application of serum formulation and DMNs was successful. In skin distribution experiments using Alexa Fluor 488 and 568 dyes as model drugs, we confirmed that the pretreated serum formulation was delivered into the skin through microchannels created by the DMNs. In vitro skin permeation and retention experiments confirmed that this novel combined application delivered more 4-n-butylresorcinol into the skin than traditional DMN-only and serum-only applications. Moreover, this combined application showed a higher efficacy in reducing patients' melanin index and hyperpigmented regions compared with the serum-only application. As combined application of DMNs on serum-treated skin can overcome both dose limitations and safety concerns, this novel approach can advance developments in transdermal drug delivery.

Original languageEnglish
Pages (from-to)2024-2031
Number of pages8
JournalMolecular Pharmaceutics
Volume14
Issue number6
DOIs
Publication statusPublished - 2017 Jun 5

Fingerprint

Skin
Serum
Pharmaceutical Preparations
Drug Compounding
Hyperpigmentation
Melanins
Drug Delivery Systems
Coloring Agents
Safety
4-n-butylresorcinol

All Science Journal Classification (ASJC) codes

  • Molecular Medicine
  • Pharmaceutical Science
  • Drug Discovery

Cite this

Kim, Suyong ; Dangol, Manita ; Kang, Geonwoo ; Lahiji, Shayan F. ; Yang, Huisuk ; Jang, Mingyu ; Ma, Yonghao ; Li, Chengguo ; Lee, Sang Gon ; Kim, Chang Hyun ; Choi, Young Wook ; Kim, So Jeong ; Ryu, Ja Hyun ; Baek, Ji Hwoon ; Koh, Jaesuk ; Jung, Hyungil. / Enhanced Transdermal Delivery by Combined Application of Dissolving Microneedle Patch on Serum-Treated Skin. In: Molecular Pharmaceutics. 2017 ; Vol. 14, No. 6. pp. 2024-2031.
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abstract = "Dissolving microneedle (DMN), a transdermal drug delivery system in which drugs are encapsulated in a biodegradable polymeric microstructure, is designed to dissolve after skin penetration and release the encapsulated drugs into the body. However, because of limited loading capacity of drugs within microsized structures, only a small dosage can be delivered, which is often insufficient for patients. We propose a novel DMN application that combines topical and DMN application simultaneously to improve skin permeation efficiency. Drugs in pretreated topical formulation and encapsulated drugs in DMN patch are delivered into the skin through microchannels created by DMN application, thus greatly increasing the delivered dose. We used 4-n-butylresorcinol to treat human hyperpigmentation and found that sequential application of serum formulation and DMNs was successful. In skin distribution experiments using Alexa Fluor 488 and 568 dyes as model drugs, we confirmed that the pretreated serum formulation was delivered into the skin through microchannels created by the DMNs. In vitro skin permeation and retention experiments confirmed that this novel combined application delivered more 4-n-butylresorcinol into the skin than traditional DMN-only and serum-only applications. Moreover, this combined application showed a higher efficacy in reducing patients' melanin index and hyperpigmented regions compared with the serum-only application. As combined application of DMNs on serum-treated skin can overcome both dose limitations and safety concerns, this novel approach can advance developments in transdermal drug delivery.",
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Kim, S, Dangol, M, Kang, G, Lahiji, SF, Yang, H, Jang, M, Ma, Y, Li, C, Lee, SG, Kim, CH, Choi, YW, Kim, SJ, Ryu, JH, Baek, JH, Koh, J & Jung, H 2017, 'Enhanced Transdermal Delivery by Combined Application of Dissolving Microneedle Patch on Serum-Treated Skin', Molecular Pharmaceutics, vol. 14, no. 6, pp. 2024-2031. https://doi.org/10.1021/acs.molpharmaceut.7b00111

Enhanced Transdermal Delivery by Combined Application of Dissolving Microneedle Patch on Serum-Treated Skin. / Kim, Suyong; Dangol, Manita; Kang, Geonwoo; Lahiji, Shayan F.; Yang, Huisuk; Jang, Mingyu; Ma, Yonghao; Li, Chengguo; Lee, Sang Gon; Kim, Chang Hyun; Choi, Young Wook; Kim, So Jeong; Ryu, Ja Hyun; Baek, Ji Hwoon; Koh, Jaesuk; Jung, Hyungil.

In: Molecular Pharmaceutics, Vol. 14, No. 6, 05.06.2017, p. 2024-2031.

Research output: Contribution to journalArticle

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T1 - Enhanced Transdermal Delivery by Combined Application of Dissolving Microneedle Patch on Serum-Treated Skin

AU - Kim, Suyong

AU - Dangol, Manita

AU - Kang, Geonwoo

AU - Lahiji, Shayan F.

AU - Yang, Huisuk

AU - Jang, Mingyu

AU - Ma, Yonghao

AU - Li, Chengguo

AU - Lee, Sang Gon

AU - Kim, Chang Hyun

AU - Choi, Young Wook

AU - Kim, So Jeong

AU - Ryu, Ja Hyun

AU - Baek, Ji Hwoon

AU - Koh, Jaesuk

AU - Jung, Hyungil

PY - 2017/6/5

Y1 - 2017/6/5

N2 - Dissolving microneedle (DMN), a transdermal drug delivery system in which drugs are encapsulated in a biodegradable polymeric microstructure, is designed to dissolve after skin penetration and release the encapsulated drugs into the body. However, because of limited loading capacity of drugs within microsized structures, only a small dosage can be delivered, which is often insufficient for patients. We propose a novel DMN application that combines topical and DMN application simultaneously to improve skin permeation efficiency. Drugs in pretreated topical formulation and encapsulated drugs in DMN patch are delivered into the skin through microchannels created by DMN application, thus greatly increasing the delivered dose. We used 4-n-butylresorcinol to treat human hyperpigmentation and found that sequential application of serum formulation and DMNs was successful. In skin distribution experiments using Alexa Fluor 488 and 568 dyes as model drugs, we confirmed that the pretreated serum formulation was delivered into the skin through microchannels created by the DMNs. In vitro skin permeation and retention experiments confirmed that this novel combined application delivered more 4-n-butylresorcinol into the skin than traditional DMN-only and serum-only applications. Moreover, this combined application showed a higher efficacy in reducing patients' melanin index and hyperpigmented regions compared with the serum-only application. As combined application of DMNs on serum-treated skin can overcome both dose limitations and safety concerns, this novel approach can advance developments in transdermal drug delivery.

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