Chen Yuan, Wang Shan, Mao Congxiu, Lu Qinyi, Zhu Xingyu, Fan Dongqi, Liu Yiping, Chen Xu, Zhan Jinglei, Yang Zixin, Ji Ping, He Qingqing, Chen Tao
The Affiliated Stomatological Hospital of Chongqing Medical University, Chongqing Key Laboratory of Oral Diseases, Chongqing Municipal Key laboratory of Oral Biomedical Engineering of Higher Education, Chongqing Municipal Health Commission Key Laboratory of Oral Biomedical Engineering, Chongqing, China.
Nat Commun. 2025 Sep 18;16(1):8321. doi: 10.1038/s41467-025-63438-7.
Hypertrophic scars are a stubborn form of dermal fibrosis that impairs quality of life. Although 5-ALA-mediated photodynamic therapy holds promise, its efficacy is undermined by poor transdermal delivery and rapid metabolism into non-photosensitive heme. Here, we introduce a "zero-waste" strategy that repurposes 5-ALA-derived heme to synergistically amplify ferroptosis. This is achieved by co-encapsulating 5-ALA and baicalin within human H-ferritin, subsequently incorporated into polyvinylpyrrolidone microneedles. The resulting system enables targeted delivery to hypertrophic scar fibroblasts with pH-responsive, programmable drug release. Upon administration, 5-ALA generates protoporphyrin IX to initiate photodynamic therapy. Baicalin is then released to induce ferroptosis and synergize with the reactive oxygen species and heme accumulated during photodynamic therapy, thereby overstimulating the HO-1-heme metabolic axis. This cascade promotes the release of Fe²⁺ and CO, further amplifying ferroptotic responses. Moreover, the ferroptotic stress triggers mitophagy and mitochondrial Fe²⁺ efflux. By harnessing 5-ALA metabolic byproducts, this strategy achieved markedly prolonged anti-scar efficacy in the female rabbit ear HS tissues, surpassing that of conventional therapies.
肥厚性瘢痕是一种顽固的皮肤纤维化形式,会损害生活质量。尽管5-氨基乙酰丙酸介导的光动力疗法前景广阔,但其经皮递送效果不佳且会迅速代谢为非光敏血红素,从而削弱了其疗效。在此,我们引入了一种“零浪费”策略,该策略将5-氨基乙酰丙酸衍生的血红素重新利用,以协同增强铁死亡。这是通过将5-氨基乙酰丙酸和黄芩苷共包封在人H-铁蛋白中,随后将其掺入聚乙烯吡咯烷酮微针中来实现的。所得系统能够通过pH响应性、可编程药物释放将药物靶向递送至肥厚性瘢痕成纤维细胞。给药后,5-氨基乙酰丙酸生成原卟啉IX以启动光动力疗法。然后释放黄芩苷以诱导铁死亡,并与光动力疗法期间积累的活性氧和血红素协同作用,从而过度刺激HO-1-血红素代谢轴。这一级联反应促进Fe²⁺和CO的释放,进一步放大铁死亡反应。此外,铁死亡应激触发线粒体自噬和线粒体Fe²⁺外流。通过利用5-氨基乙酰丙酸的代谢副产物,该策略在雌性兔耳肥厚性瘢痕组织中实现了显著延长的抗瘢痕疗效,超过了传统疗法。