The pilosebaceous unit is the collective form of a hair follicle, hair shaft, and sebaceous gland. Within the skin, this three-dimensional composite shows a distinctive biochemistry, metabolism, and immunology. Presently, most researchers in this area are focused on the hair follicles, as they see these as a potential pathway for both localized and systemic delivery of various chemotherapeutics. Better understanding of the configuration of the hair follicle is mulled over in order to design rational drug formulations to achieve targeted follicular delivery. Targeted drug delivery may enhance the efficacy of current therapeutics to treat diseases of follicular origin. The present review covers follicular drug delivery with the potential to target the pilosebaceous unit.