Acne vulgaris (AV) is a prevalent skin condition affecting the cutaneous appendages and hair follicles. It is particularly frequent among young adults aged 12 to 25 years. Its incidence varies substantially across countries and according to different ethnicities, with notable impacts on mental health and social functioning. Conventional treatments often cause disruption on the skin barrier, leading to undesirable effects and poor adherence. Recent research has focused on hair follicles (HF) as a potential route for targeted drug delivery to address follicle-related disorders, such as AV. Nanotechnology-based delivery systems offer promising avenues for enhancing drug penetration and efficacy while minimizing adverse effects. However, optimal nanoparticle properties for HF deposition and the influence of secondary delivery vehicles remain subjects of debate. This review explores recent advancements in HF-targeted drug delivery, highlighting the potential of nanocarriers in revolutionizing acne treatment.