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Recent studies have shown that biologically active macromolecules can help regenerate hair, providing a potential solution for current hair regeneration therapies. This review examines the latest developments in the use of macromolecules for the treatment of hair loss. The fundamental principles of hair follicle (HF) morphogenesis, hair shaft (HS) development, hair cycle regulation, and alopecia have been introduced. Microneedle (MN) and nanoparticle (NP) delivery systems are innovative treatments for hair loss. Additionally, the application of macromolecule\u2010based tissue\u2010engineered scaffolds for the in vitro and in vivo neogenesis of HFs is discussed. Furthermore, a new research direction is explored wherein artificial skin platforms are adopted as a promising screening method for hair loss treatment drugs. 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