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

Abstract

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.