Solvent-free polycaprolactone dissolving microneedles generated via the thermal melting method for the sustained release of capsaicin

Jaehong Eum; Youseong Kim; Daniel Junmin Um; Jiwoo Shin; Huisuk Yang; Hyungil Jung

doi:10.3390/mi12020167

Solvent-free polycaprolactone dissolving microneedles generated via the thermal melting method for the sustained release of capsaicin

Jaehong Eum, Youseong Kim, Daniel Junmin Um, Jiwoo Shin, Huisuk Yang, Hyungil Jung

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

8 Citations (Scopus)

Abstract

(1) Background: Dissolving microneedles (DMNs), a transdermal drug delivery system, have been developed to treat various diseases in a minimally invasive, painless manner. However, the currently available DMNs are based on burst release systems due to their hydrophilic backbone polymer. Although hydrophobic biodegradable polymers have been employed on DMNs for sustained release, dissolution in an organic solvent is required for fabrication of such DMNs. (2) Method: To overcome the aforementioned limitation, novel separable polycaprolactone (PCL) DMNs (SPCL-DMNs) were developed to implant a PCL-encapsulated drug into the skin. PCL is highly hydrophobic, degrades over a long time, and has a low melting point. Under thermal melting, PCL encapsulated capsaicin and could be fabricated into a DMN without the risk of toxicity from an organic solvent. (3) Results: Optimized SPCL-DMNs, containing PCL (height 498.3 ± 5.8 µm) encapsulating 86.66 ± 1.13 µg capsaicin with a 10% (w/v) polyvinyl alcohol and 20% (w/v) polyvinylpyrrolidone mixture as a base polymer, were generated. Assessment of the drug release profile revealed that this system could sustainably release capsaicin for 15 days from PCL being implanted in porcine skin. (4) Conclusion: The implantable SPCL-DMN developed here has the potential for future development of toxicity-free, sustained release DMNs.

Original language	English
Article number	167
Journal	Micromachines
Volume	12
Issue number	2
DOIs	https://doi.org/10.3390/mi12020167
Publication status	Published - 2021 Feb

Bibliographical note

Funding Information:
Funding: This reasearch was equally supported by a grant of the Korea Health Technology R&D Project through the Korea Health Industry Development Institute (KHIDI), funded by the Ministry of Health & Welfare, Republic of Korea (grant number: HI16C0625), by the National Research Foundation of Korea (NRF) grant funded by the Korea government (MSIT) (grant number: 2020M3E5D8108104), and by Brain Korea 21 (BK21) program/Y.K. and J.S. are fellowship awardees of the BK21 program.

Publisher Copyright:
© 2021 by the authors. Licensee MDPI, Basel, Switzerland.

All Science Journal Classification (ASJC) codes

Control and Systems Engineering
Mechanical Engineering
Electrical and Electronic Engineering

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10.3390/mi12020167

Cite this

@article{8b69a54c54de4d70baef22a2bc365c12,

title = "Solvent-free polycaprolactone dissolving microneedles generated via the thermal melting method for the sustained release of capsaicin",

abstract = "(1) Background: Dissolving microneedles (DMNs), a transdermal drug delivery system, have been developed to treat various diseases in a minimally invasive, painless manner. However, the currently available DMNs are based on burst release systems due to their hydrophilic backbone polymer. Although hydrophobic biodegradable polymers have been employed on DMNs for sustained release, dissolution in an organic solvent is required for fabrication of such DMNs. (2) Method: To overcome the aforementioned limitation, novel separable polycaprolactone (PCL) DMNs (SPCL-DMNs) were developed to implant a PCL-encapsulated drug into the skin. PCL is highly hydrophobic, degrades over a long time, and has a low melting point. Under thermal melting, PCL encapsulated capsaicin and could be fabricated into a DMN without the risk of toxicity from an organic solvent. (3) Results: Optimized SPCL-DMNs, containing PCL (height 498.3 ± 5.8 µm) encapsulating 86.66 ± 1.13 µg capsaicin with a 10% (w/v) polyvinyl alcohol and 20% (w/v) polyvinylpyrrolidone mixture as a base polymer, were generated. Assessment of the drug release profile revealed that this system could sustainably release capsaicin for 15 days from PCL being implanted in porcine skin. (4) Conclusion: The implantable SPCL-DMN developed here has the potential for future development of toxicity-free, sustained release DMNs.",

author = "Jaehong Eum and Youseong Kim and Um, {Daniel Junmin} and Jiwoo Shin and Huisuk Yang and Hyungil Jung",

note = "Funding Information: Funding: This reasearch was equally supported by a grant of the Korea Health Technology R&D Project through the Korea Health Industry Development Institute (KHIDI), funded by the Ministry of Health & Welfare, Republic of Korea (grant number: HI16C0625), by the National Research Foundation of Korea (NRF) grant funded by the Korea government (MSIT) (grant number: 2020M3E5D8108104), and by Brain Korea 21 (BK21) program/Y.K. and J.S. are fellowship awardees of the BK21 program. Publisher Copyright: {\textcopyright} 2021 by the authors. Licensee MDPI, Basel, Switzerland.",

year = "2021",

month = feb,

doi = "10.3390/mi12020167",

language = "English",

volume = "12",

journal = "Micromachines",

issn = "2072-666X",

publisher = "Multidisciplinary Digital Publishing Institute (MDPI)",

number = "2",

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TY - JOUR

T1 - Solvent-free polycaprolactone dissolving microneedles generated via the thermal melting method for the sustained release of capsaicin

AU - Eum, Jaehong

AU - Kim, Youseong

AU - Um, Daniel Junmin

AU - Shin, Jiwoo

AU - Yang, Huisuk

AU - Jung, Hyungil

N1 - Funding Information: Funding: This reasearch was equally supported by a grant of the Korea Health Technology R&D Project through the Korea Health Industry Development Institute (KHIDI), funded by the Ministry of Health & Welfare, Republic of Korea (grant number: HI16C0625), by the National Research Foundation of Korea (NRF) grant funded by the Korea government (MSIT) (grant number: 2020M3E5D8108104), and by Brain Korea 21 (BK21) program/Y.K. and J.S. are fellowship awardees of the BK21 program. Publisher Copyright: © 2021 by the authors. Licensee MDPI, Basel, Switzerland.

PY - 2021/2

Y1 - 2021/2

N2 - (1) Background: Dissolving microneedles (DMNs), a transdermal drug delivery system, have been developed to treat various diseases in a minimally invasive, painless manner. However, the currently available DMNs are based on burst release systems due to their hydrophilic backbone polymer. Although hydrophobic biodegradable polymers have been employed on DMNs for sustained release, dissolution in an organic solvent is required for fabrication of such DMNs. (2) Method: To overcome the aforementioned limitation, novel separable polycaprolactone (PCL) DMNs (SPCL-DMNs) were developed to implant a PCL-encapsulated drug into the skin. PCL is highly hydrophobic, degrades over a long time, and has a low melting point. Under thermal melting, PCL encapsulated capsaicin and could be fabricated into a DMN without the risk of toxicity from an organic solvent. (3) Results: Optimized SPCL-DMNs, containing PCL (height 498.3 ± 5.8 µm) encapsulating 86.66 ± 1.13 µg capsaicin with a 10% (w/v) polyvinyl alcohol and 20% (w/v) polyvinylpyrrolidone mixture as a base polymer, were generated. Assessment of the drug release profile revealed that this system could sustainably release capsaicin for 15 days from PCL being implanted in porcine skin. (4) Conclusion: The implantable SPCL-DMN developed here has the potential for future development of toxicity-free, sustained release DMNs.

AB - (1) Background: Dissolving microneedles (DMNs), a transdermal drug delivery system, have been developed to treat various diseases in a minimally invasive, painless manner. However, the currently available DMNs are based on burst release systems due to their hydrophilic backbone polymer. Although hydrophobic biodegradable polymers have been employed on DMNs for sustained release, dissolution in an organic solvent is required for fabrication of such DMNs. (2) Method: To overcome the aforementioned limitation, novel separable polycaprolactone (PCL) DMNs (SPCL-DMNs) were developed to implant a PCL-encapsulated drug into the skin. PCL is highly hydrophobic, degrades over a long time, and has a low melting point. Under thermal melting, PCL encapsulated capsaicin and could be fabricated into a DMN without the risk of toxicity from an organic solvent. (3) Results: Optimized SPCL-DMNs, containing PCL (height 498.3 ± 5.8 µm) encapsulating 86.66 ± 1.13 µg capsaicin with a 10% (w/v) polyvinyl alcohol and 20% (w/v) polyvinylpyrrolidone mixture as a base polymer, were generated. Assessment of the drug release profile revealed that this system could sustainably release capsaicin for 15 days from PCL being implanted in porcine skin. (4) Conclusion: The implantable SPCL-DMN developed here has the potential for future development of toxicity-free, sustained release DMNs.

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U2 - 10.3390/mi12020167

DO - 10.3390/mi12020167

M3 - Article

AN - SCOPUS:85101242624

SN - 2072-666X

VL - 12

JO - Micromachines

JF - Micromachines

IS - 2

M1 - 167

ER -

Solvent-free polycaprolactone dissolving microneedles generated via the thermal melting method for the sustained release of capsaicin

Abstract

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