Proteoglycan Mimetics-based Bioactive Microneedles with Regulation Capacities of Inflammatory Microenvironment and Lipid Metabolism for Acne Treatment

Although microneedles (MNs) can deliver bacteriostats for acne treatment, the limited regulation of inflammatory microenvironment and lipid metabolism hinders the therapeutic effect on severe acne. Herein, we develop antimicrobial and anti-inflammatory peptides-laden MN (HMC-PEP MN) with a proteoglycan-mimetic peptide-grafted comb polymer as MN matrix, which effectively treats acne via regulation of both inflammatory microenvironment and lipid metabolism.

Specifically, HMC-PEP MN inhibits the expression of pro-inflammatory factors by decreasing TREM2/M2 macrophage ratio in rabbit ear acne model. Integrative analyses of transcriptomic and metabolomic reveal that HMC-PEP MN effectively reduces sebaceous secretion, pro-inflammatory signal transduction, sustained proliferation and differentiation of keratinocytes via inhibition of the IGF1/IGF1R/PI3K/AKT/mTOR signaling pathway.