Bilayer dissolving microneedle array containing 5-fluorouracil and triamcinolone with biphasic release profile for hypertrophic scar therapy
Hypertrophic scar (HS) is an undesirable skin abnormality following deep burns or operations. Although intralesional multi-injection with the suspension of triamcinolone acetonide (TA) and 5-fluorouracil (5-Fu) has exhibited great promise to HS treatment in clinical, the difference of metabolic beha...
Main Authors: | , , , , , , |
---|---|
Format: | Article |
Language: | English |
Published: |
KeAi Communications Co., Ltd.
2021-08-01
|
Series: | Bioactive Materials |
Subjects: | |
Online Access: | http://www.sciencedirect.com/science/article/pii/S2452199X21000256 |
id |
doaj-e92596192d004429b05198c7339d4cce |
---|---|
record_format |
Article |
spelling |
doaj-e92596192d004429b05198c7339d4cce2021-05-08T04:23:37ZengKeAi Communications Co., Ltd.Bioactive Materials2452-199X2021-08-016824002411Bilayer dissolving microneedle array containing 5-fluorouracil and triamcinolone with biphasic release profile for hypertrophic scar therapyBeibei Yang0Yating Dong1Yifeng Shen2Ailin Hou3Guilan Quan4Xin Pan5Chuanbin Wu6School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, 510006, ChinaSchool of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, 510006, ChinaSchool of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, 510006, ChinaSchool of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, 510006, ChinaCollege of Pharmacy, Jinan University, Guangzhou, 510632, China; Corresponding author.School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, 510006, China; Corresponding author.College of Pharmacy, Jinan University, Guangzhou, 510632, ChinaHypertrophic scar (HS) is an undesirable skin abnormality following deep burns or operations. Although intralesional multi-injection with the suspension of triamcinolone acetonide (TA) and 5-fluorouracil (5-Fu) has exhibited great promise to HS treatment in clinical, the difference of metabolic behavior between TA and 5-Fu remarkably compromised the treatment efficacy. Besides, the traditional injection with great pain is highly dependent on the skill of the experts, which results in poor compliance. Herein, a bilayer dissolving microneedle (BMN) containing TA and 5-Fu (TA-5-Fu-BMN) with biphasic release profile was designed for HS therapy. Equipped with several micro-scale needle tips, the BMN could be self-pressed into the HS with uniform drug distribution and less pain. Both in vitro permeation and in vivo HS retention tests revealed that TA and 5-Fu could coexist in the scar tissue for a sufficient time period due to the well-designed biphasic release property. Subsequently, the rabbit ear HS model was established to assess therapeutic efficacy. The histological analysis showed that TA-5-Fu-BMN could significantly reduce abnormal fibroblast proliferation and collagen fiber deposition. It was also found that the value of scar elevation index was ameliorated to a basal level, together with the downregulation of mRNA and protein expression of Collagen I (Col I) and transforming growth factor-β1 (TGF-β1) after application of TA-5-Fu-BMN. In conclusion, the BMN with biphasic release profiles could serve as a potential strategy for HS treatment providing both convenient administrations as well as controlled drug release behavior.http://www.sciencedirect.com/science/article/pii/S2452199X21000256Hypertrophic scarBilayer microneedleBiphasic releaseTriamcinolone acetonide5-Fluorouracil |
collection |
DOAJ |
language |
English |
format |
Article |
sources |
DOAJ |
author |
Beibei Yang Yating Dong Yifeng Shen Ailin Hou Guilan Quan Xin Pan Chuanbin Wu |
spellingShingle |
Beibei Yang Yating Dong Yifeng Shen Ailin Hou Guilan Quan Xin Pan Chuanbin Wu Bilayer dissolving microneedle array containing 5-fluorouracil and triamcinolone with biphasic release profile for hypertrophic scar therapy Bioactive Materials Hypertrophic scar Bilayer microneedle Biphasic release Triamcinolone acetonide 5-Fluorouracil |
author_facet |
Beibei Yang Yating Dong Yifeng Shen Ailin Hou Guilan Quan Xin Pan Chuanbin Wu |
author_sort |
Beibei Yang |
title |
Bilayer dissolving microneedle array containing 5-fluorouracil and triamcinolone with biphasic release profile for hypertrophic scar therapy |
title_short |
Bilayer dissolving microneedle array containing 5-fluorouracil and triamcinolone with biphasic release profile for hypertrophic scar therapy |
title_full |
Bilayer dissolving microneedle array containing 5-fluorouracil and triamcinolone with biphasic release profile for hypertrophic scar therapy |
title_fullStr |
Bilayer dissolving microneedle array containing 5-fluorouracil and triamcinolone with biphasic release profile for hypertrophic scar therapy |
title_full_unstemmed |
Bilayer dissolving microneedle array containing 5-fluorouracil and triamcinolone with biphasic release profile for hypertrophic scar therapy |
title_sort |
bilayer dissolving microneedle array containing 5-fluorouracil and triamcinolone with biphasic release profile for hypertrophic scar therapy |
publisher |
KeAi Communications Co., Ltd. |
series |
Bioactive Materials |
issn |
2452-199X |
publishDate |
2021-08-01 |
description |
Hypertrophic scar (HS) is an undesirable skin abnormality following deep burns or operations. Although intralesional multi-injection with the suspension of triamcinolone acetonide (TA) and 5-fluorouracil (5-Fu) has exhibited great promise to HS treatment in clinical, the difference of metabolic behavior between TA and 5-Fu remarkably compromised the treatment efficacy. Besides, the traditional injection with great pain is highly dependent on the skill of the experts, which results in poor compliance. Herein, a bilayer dissolving microneedle (BMN) containing TA and 5-Fu (TA-5-Fu-BMN) with biphasic release profile was designed for HS therapy. Equipped with several micro-scale needle tips, the BMN could be self-pressed into the HS with uniform drug distribution and less pain. Both in vitro permeation and in vivo HS retention tests revealed that TA and 5-Fu could coexist in the scar tissue for a sufficient time period due to the well-designed biphasic release property. Subsequently, the rabbit ear HS model was established to assess therapeutic efficacy. The histological analysis showed that TA-5-Fu-BMN could significantly reduce abnormal fibroblast proliferation and collagen fiber deposition. It was also found that the value of scar elevation index was ameliorated to a basal level, together with the downregulation of mRNA and protein expression of Collagen I (Col I) and transforming growth factor-β1 (TGF-β1) after application of TA-5-Fu-BMN. In conclusion, the BMN with biphasic release profiles could serve as a potential strategy for HS treatment providing both convenient administrations as well as controlled drug release behavior. |
topic |
Hypertrophic scar Bilayer microneedle Biphasic release Triamcinolone acetonide 5-Fluorouracil |
url |
http://www.sciencedirect.com/science/article/pii/S2452199X21000256 |
work_keys_str_mv |
AT beibeiyang bilayerdissolvingmicroneedlearraycontaining5fluorouracilandtriamcinolonewithbiphasicreleaseprofileforhypertrophicscartherapy AT yatingdong bilayerdissolvingmicroneedlearraycontaining5fluorouracilandtriamcinolonewithbiphasicreleaseprofileforhypertrophicscartherapy AT yifengshen bilayerdissolvingmicroneedlearraycontaining5fluorouracilandtriamcinolonewithbiphasicreleaseprofileforhypertrophicscartherapy AT ailinhou bilayerdissolvingmicroneedlearraycontaining5fluorouracilandtriamcinolonewithbiphasicreleaseprofileforhypertrophicscartherapy AT guilanquan bilayerdissolvingmicroneedlearraycontaining5fluorouracilandtriamcinolonewithbiphasicreleaseprofileforhypertrophicscartherapy AT xinpan bilayerdissolvingmicroneedlearraycontaining5fluorouracilandtriamcinolonewithbiphasicreleaseprofileforhypertrophicscartherapy AT chuanbinwu bilayerdissolvingmicroneedlearraycontaining5fluorouracilandtriamcinolonewithbiphasicreleaseprofileforhypertrophicscartherapy |
_version_ |
1721455095432871936 |