Self-assembled arginine-based eutectogel microneedles as novel transdermal delivery system for pigmentation treatment

An efficient and patient-friendly strategy for administering skin pigmentation is achieved through microneedles (MNs) -mediated drug delivery into the dermal interstitium across the stratum corneum. In this work, we design a eutectogel to fabricate dissolving MNs delivery system, which were self-ass...

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Main Authors: Hui Ma, Yier Li, Qiufeng Yao, Ruixiu Qin, Yanan Wang, Wenhui Wu, Hui Luo, Qi Zhao, Hua Ye, Kefeng Wu
Format: Article
Language:English
Published: Elsevier 2025-06-01
Series:Giant
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Online Access:http://www.sciencedirect.com/science/article/pii/S2666542525000062
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author Hui Ma
Yier Li
Qiufeng Yao
Ruixiu Qin
Yanan Wang
Wenhui Wu
Hui Luo
Qi Zhao
Hua Ye
Kefeng Wu
author_facet Hui Ma
Yier Li
Qiufeng Yao
Ruixiu Qin
Yanan Wang
Wenhui Wu
Hui Luo
Qi Zhao
Hua Ye
Kefeng Wu
author_sort Hui Ma
collection DOAJ
description An efficient and patient-friendly strategy for administering skin pigmentation is achieved through microneedles (MNs) -mediated drug delivery into the dermal interstitium across the stratum corneum. In this work, we design a eutectogel to fabricate dissolving MNs delivery system, which were self-assembled from small molecules of arginine and sorbitol driven by hydrogen bonding interaction. The hydrogen bond-network structure conferred the arginine-sorbitol eutectogel (AsE) MNs with sufficient mechanical properties, which enable it easily pierce the thickened stratum corneum of the skin and directly deliver drugs into the deep skin lesions. Moreover, the unique eutectogel exhibits super hydrophilic properties and makes the AsE/MNs display completely dissolution and diffuse drugs rapidly. The AsE/MNs exhibit high biocompatibility and degradability in vivo and do not cause toxicity or irritation when being applied. AsE/MNs possesses remarkable drug loading capacity and stability, moreover, the permeated amounts of rutin on mice skin in the AsE/MNs was more than 15 times enhancement over that of the rutin solution group in vitro. Furthermore, the results of pharmacodynamic study in vivo demonstrated that AsE/MNs loading rutin could effectively prevent the skin pigmentation and tissue damage induced by UV irradiation. Overall, this work validated that AsE/MNs are a valuable platform for improving the transdermal bioavailability of drugs.
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spelling doaj-art-11e0f0e157a94aefbc1d5c53d78ca0282025-08-20T02:09:11ZengElsevierGiant2666-54252025-06-012310035710.1016/j.giant.2025.100357Self-assembled arginine-based eutectogel microneedles as novel transdermal delivery system for pigmentation treatmentHui Ma0Yier Li1Qiufeng Yao2Ruixiu Qin3Yanan Wang4Wenhui Wu5Hui Luo6Qi Zhao7Hua Ye8Kefeng Wu9School of Ocean and Tropical Medicine, Guangdong Medical University, Zhanjiang 524023, China; Department of Marine Bio-Pharmacology, College of Food Science and Technology, Shanghai Ocean University, Shanghai 201306, ChinaSchool of Ocean and Tropical Medicine, Guangdong Medical University, Zhanjiang 524023, China; The Marine Biomedical Research Institute of Guangdong Zhanjiang, Zhanjiang 524023, ChinaSchool of Ocean and Tropical Medicine, Guangdong Medical University, Zhanjiang 524023, China; The Marine Biomedical Research Institute of Guangdong Zhanjiang, Zhanjiang 524023, ChinaSchool of Ocean and Tropical Medicine, Guangdong Medical University, Zhanjiang 524023, China; The Marine Biomedical Research Institute of Guangdong Zhanjiang, Zhanjiang 524023, ChinaCollege of Life Sciences, Jiangxi Science and Technology Normal University, Nanchang 330013, Jiangxi, ChinaDepartment of Marine Bio-Pharmacology, College of Food Science and Technology, Shanghai Ocean University, Shanghai 201306, ChinaSchool of Ocean and Tropical Medicine, Guangdong Medical University, Zhanjiang 524023, China; The Marine Biomedical Research Institute of Guangdong Zhanjiang, Zhanjiang 524023, ChinaSchool of Ocean and Tropical Medicine, Guangdong Medical University, Zhanjiang 524023, China; The Marine Biomedical Research Institute of Guangdong Zhanjiang, Zhanjiang 524023, China; Corresponding authors at: School of Ocean and Tropical Medicine, Guangdong Medical University, Zhanjiang 524023, China.School of Ocean and Tropical Medicine, Guangdong Medical University, Zhanjiang 524023, China; The Marine Biomedical Research Institute of Guangdong Zhanjiang, Zhanjiang 524023, China; Corresponding authors at: School of Ocean and Tropical Medicine, Guangdong Medical University, Zhanjiang 524023, China.School of Ocean and Tropical Medicine, Guangdong Medical University, Zhanjiang 524023, China; The Marine Biomedical Research Institute of Guangdong Zhanjiang, Zhanjiang 524023, China; Corresponding authors at: School of Ocean and Tropical Medicine, Guangdong Medical University, Zhanjiang 524023, China.An efficient and patient-friendly strategy for administering skin pigmentation is achieved through microneedles (MNs) -mediated drug delivery into the dermal interstitium across the stratum corneum. In this work, we design a eutectogel to fabricate dissolving MNs delivery system, which were self-assembled from small molecules of arginine and sorbitol driven by hydrogen bonding interaction. The hydrogen bond-network structure conferred the arginine-sorbitol eutectogel (AsE) MNs with sufficient mechanical properties, which enable it easily pierce the thickened stratum corneum of the skin and directly deliver drugs into the deep skin lesions. Moreover, the unique eutectogel exhibits super hydrophilic properties and makes the AsE/MNs display completely dissolution and diffuse drugs rapidly. The AsE/MNs exhibit high biocompatibility and degradability in vivo and do not cause toxicity or irritation when being applied. AsE/MNs possesses remarkable drug loading capacity and stability, moreover, the permeated amounts of rutin on mice skin in the AsE/MNs was more than 15 times enhancement over that of the rutin solution group in vitro. Furthermore, the results of pharmacodynamic study in vivo demonstrated that AsE/MNs loading rutin could effectively prevent the skin pigmentation and tissue damage induced by UV irradiation. Overall, this work validated that AsE/MNs are a valuable platform for improving the transdermal bioavailability of drugs.http://www.sciencedirect.com/science/article/pii/S2666542525000062EutectogelMicroneedleSelf-assembledHydrogen bondingDrug delivery
spellingShingle Hui Ma
Yier Li
Qiufeng Yao
Ruixiu Qin
Yanan Wang
Wenhui Wu
Hui Luo
Qi Zhao
Hua Ye
Kefeng Wu
Self-assembled arginine-based eutectogel microneedles as novel transdermal delivery system for pigmentation treatment
Giant
Eutectogel
Microneedle
Self-assembled
Hydrogen bonding
Drug delivery
title Self-assembled arginine-based eutectogel microneedles as novel transdermal delivery system for pigmentation treatment
title_full Self-assembled arginine-based eutectogel microneedles as novel transdermal delivery system for pigmentation treatment
title_fullStr Self-assembled arginine-based eutectogel microneedles as novel transdermal delivery system for pigmentation treatment
title_full_unstemmed Self-assembled arginine-based eutectogel microneedles as novel transdermal delivery system for pigmentation treatment
title_short Self-assembled arginine-based eutectogel microneedles as novel transdermal delivery system for pigmentation treatment
title_sort self assembled arginine based eutectogel microneedles as novel transdermal delivery system for pigmentation treatment
topic Eutectogel
Microneedle
Self-assembled
Hydrogen bonding
Drug delivery
url http://www.sciencedirect.com/science/article/pii/S2666542525000062
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