Drug-based monotherapy provides limited clinical benefits in polygenic disorders, such as androgenetic alopecia. Possible benefits must be measured against non-trivial risks of negative side effects. Several well-controlled, peer-reviewed, basic science studies have demonstrated novel mechanisms of action and potential utility for natural-based phytochemicals in the treatment of androgen-mediated disorders, including androgenetic alopecia. Yet, due to phytochemical instability, volatility, and incompatibility, the bridge from in vitro potential to clinical efficacy remains largely unmet. Recent advances in nanomaterial manipulation provide enhanced platforms, such as cyclodextrins, in which these phytochemicals may be enveloped and delivered without triggering the loss of intended function. Unexpected, positive results of an uncontrolled case series for a cyclodextrin-enabled, natural-based formula containing γ linolenic acid, β-Sitosterol, epigallocatechin gallate, and genistein, administered concomitantly via oral and topical form in two androgenetic alopecia-affected, male subjects over the course of 270 days were found. At baseline, significant baldness in the vertex scalp of both subjects was observed. Subsequent 90-day time points demonstrated marked hair thickening. On treatment day 270 (conclusion), scalp hair loss was no longer evident in either patient. Particularly in the setting of a disorders, such as androgenetic alopecia, nano-complexed, botanically-based compositions may offer beneficial adjunctives or alternatives to traditional drug-based/surgical medical treatments.