Autonomous drug delivery and scar microenvironment remodeling using micromotor-driven microneedles for hypertrophic scars therapy

Hypertrophic scar is a fibrous hyperplastic disorder that arises from skin injuries. The current therapeutic modalities are constrained by the dense and rigid scar tissue which impedes effective drug delivery. Additionally, insufficient autophagic activity in fibroblasts hinders their apoptosis, lea...

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Main Authors: Ting Wen, Yanping Fu, Xiangting Yi, Ying Sun, Wanchen Zhao, Chaonan Shi, Ziyao Chang, Beibei Yang, Shuling Li, Chao Lu, Tingting Peng, Chuanbin Wu, Xin Pan, Guilan Quan
Format: Article
Language:English
Published: Elsevier 2025-07-01
Series:Acta Pharmaceutica Sinica B
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Online Access:http://www.sciencedirect.com/science/article/pii/S2211383525003235
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author Ting Wen
Yanping Fu
Xiangting Yi
Ying Sun
Wanchen Zhao
Chaonan Shi
Ziyao Chang
Beibei Yang
Shuling Li
Chao Lu
Tingting Peng
Chuanbin Wu
Xin Pan
Guilan Quan
author_facet Ting Wen
Yanping Fu
Xiangting Yi
Ying Sun
Wanchen Zhao
Chaonan Shi
Ziyao Chang
Beibei Yang
Shuling Li
Chao Lu
Tingting Peng
Chuanbin Wu
Xin Pan
Guilan Quan
author_sort Ting Wen
collection DOAJ
description Hypertrophic scar is a fibrous hyperplastic disorder that arises from skin injuries. The current therapeutic modalities are constrained by the dense and rigid scar tissue which impedes effective drug delivery. Additionally, insufficient autophagic activity in fibroblasts hinders their apoptosis, leading to excessive matrix deposition. Here, we developed an active microneedle (MN) system to overcome these challenges by integrating micromotor-driven drug delivery with autophagy regulation to remodel the scar microenvironment. Specifically, sodium bicarbonate and citric acid were introduced into the MNs as a built-in engine to generate CO2 bubbles, thereby enabling enhanced lateral and vertical drug diffusion into dense scar tissue. The system concurrently encapsulated curcumin (Cur), an autophagy activator, and triamcinolone acetonide (TA), synergistically inducing fibroblast apoptosis by upregulating autophagic activity. In vitro studies demonstrated that active MNs achieved efficient drug penetration within isolated scar tissue. The rabbit hypertrophic scar model revealed that TA-Cur MNs significantly reduced the scar elevation index, suppressed collagen I and transforming growth factor-β1 (TGF-β1) expression, and elevated LC3 protein levels. These findings highlight the potential of the active MN system as an efficacious platform for autonomous augmented drug delivery and autophagy-targeted therapy in fibrotic disorder treatments.
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spelling doaj-art-49ee70eae712480883f731c83040bb272025-08-20T03:17:24ZengElsevierActa Pharmaceutica Sinica B2211-38352025-07-011573738375510.1016/j.apsb.2025.05.017Autonomous drug delivery and scar microenvironment remodeling using micromotor-driven microneedles for hypertrophic scars therapyTing Wen0Yanping Fu1Xiangting Yi2Ying Sun3Wanchen Zhao4Chaonan Shi5Ziyao Chang6Beibei Yang7Shuling Li8Chao Lu9Tingting Peng10Chuanbin Wu11Xin Pan12Guilan Quan13School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, ChinaState Key Laboratory of Bioactive Molecules and Druggability Assessment, Guangdong Basic Research Center of Excellence for Natural Bioactive Molecules and Discovery of Innovative Drugs, College of Pharmacy, Jinan University, Guangzhou 510632, ChinaState Key Laboratory of Bioactive Molecules and Druggability Assessment, Guangdong Basic Research Center of Excellence for Natural Bioactive Molecules and Discovery of Innovative Drugs, College of Pharmacy, Jinan University, Guangzhou 510632, ChinaSchool of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, ChinaState Key Laboratory of Bioactive Molecules and Druggability Assessment, Guangdong Basic Research Center of Excellence for Natural Bioactive Molecules and Discovery of Innovative Drugs, College of Pharmacy, Jinan University, Guangzhou 510632, ChinaState Key Laboratory of Bioactive Molecules and Druggability Assessment, Guangdong Basic Research Center of Excellence for Natural Bioactive Molecules and Discovery of Innovative Drugs, College of Pharmacy, Jinan University, Guangzhou 510632, ChinaSchool of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, ChinaSchool of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, ChinaState Key Laboratory of Bioactive Molecules and Druggability Assessment, Guangdong Basic Research Center of Excellence for Natural Bioactive Molecules and Discovery of Innovative Drugs, College of Pharmacy, Jinan University, Guangzhou 510632, ChinaState Key Laboratory of Bioactive Molecules and Druggability Assessment, Guangdong Basic Research Center of Excellence for Natural Bioactive Molecules and Discovery of Innovative Drugs, College of Pharmacy, Jinan University, Guangzhou 510632, ChinaState Key Laboratory of Bioactive Molecules and Druggability Assessment, Guangdong Basic Research Center of Excellence for Natural Bioactive Molecules and Discovery of Innovative Drugs, College of Pharmacy, Jinan University, Guangzhou 510632, ChinaState Key Laboratory of Bioactive Molecules and Druggability Assessment, Guangdong Basic Research Center of Excellence for Natural Bioactive Molecules and Discovery of Innovative Drugs, College of Pharmacy, Jinan University, Guangzhou 510632, China; Jiangmen Wuyi Hospital of Traditional Chinese Medicine, Affiliated Jiangmen Traditional Chinese Medicine Hospital of Jinan University, Jiangmen 529031, ChinaSchool of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China; Corresponding authors.State Key Laboratory of Bioactive Molecules and Druggability Assessment, Guangdong Basic Research Center of Excellence for Natural Bioactive Molecules and Discovery of Innovative Drugs, College of Pharmacy, Jinan University, Guangzhou 510632, China; Corresponding authors.Hypertrophic scar is a fibrous hyperplastic disorder that arises from skin injuries. The current therapeutic modalities are constrained by the dense and rigid scar tissue which impedes effective drug delivery. Additionally, insufficient autophagic activity in fibroblasts hinders their apoptosis, leading to excessive matrix deposition. Here, we developed an active microneedle (MN) system to overcome these challenges by integrating micromotor-driven drug delivery with autophagy regulation to remodel the scar microenvironment. Specifically, sodium bicarbonate and citric acid were introduced into the MNs as a built-in engine to generate CO2 bubbles, thereby enabling enhanced lateral and vertical drug diffusion into dense scar tissue. The system concurrently encapsulated curcumin (Cur), an autophagy activator, and triamcinolone acetonide (TA), synergistically inducing fibroblast apoptosis by upregulating autophagic activity. In vitro studies demonstrated that active MNs achieved efficient drug penetration within isolated scar tissue. The rabbit hypertrophic scar model revealed that TA-Cur MNs significantly reduced the scar elevation index, suppressed collagen I and transforming growth factor-β1 (TGF-β1) expression, and elevated LC3 protein levels. These findings highlight the potential of the active MN system as an efficacious platform for autonomous augmented drug delivery and autophagy-targeted therapy in fibrotic disorder treatments.http://www.sciencedirect.com/science/article/pii/S2211383525003235Hypertrophic scarMicroneedlesAutonomous drug deliveryDrug diffusionAutophagy regulationFibroblast apoptosis
spellingShingle Ting Wen
Yanping Fu
Xiangting Yi
Ying Sun
Wanchen Zhao
Chaonan Shi
Ziyao Chang
Beibei Yang
Shuling Li
Chao Lu
Tingting Peng
Chuanbin Wu
Xin Pan
Guilan Quan
Autonomous drug delivery and scar microenvironment remodeling using micromotor-driven microneedles for hypertrophic scars therapy
Acta Pharmaceutica Sinica B
Hypertrophic scar
Microneedles
Autonomous drug delivery
Drug diffusion
Autophagy regulation
Fibroblast apoptosis
title Autonomous drug delivery and scar microenvironment remodeling using micromotor-driven microneedles for hypertrophic scars therapy
title_full Autonomous drug delivery and scar microenvironment remodeling using micromotor-driven microneedles for hypertrophic scars therapy
title_fullStr Autonomous drug delivery and scar microenvironment remodeling using micromotor-driven microneedles for hypertrophic scars therapy
title_full_unstemmed Autonomous drug delivery and scar microenvironment remodeling using micromotor-driven microneedles for hypertrophic scars therapy
title_short Autonomous drug delivery and scar microenvironment remodeling using micromotor-driven microneedles for hypertrophic scars therapy
title_sort autonomous drug delivery and scar microenvironment remodeling using micromotor driven microneedles for hypertrophic scars therapy
topic Hypertrophic scar
Microneedles
Autonomous drug delivery
Drug diffusion
Autophagy regulation
Fibroblast apoptosis
url http://www.sciencedirect.com/science/article/pii/S2211383525003235
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