Provided are: a pharmaceutical composition including a gamma-cyclodextrin-based polymer, for prevention and treatment of diseases related to cholesterol metabolism dysregulation; and use thereof. The pharmaceutical composition including a gamma-cyclodextrin polymer for prevention or treatment of diseases related to cholesterol metabolism dysregulation, according to an embodiment, by including the gamma-cyclodextrin-based polymer, may minimize extraction of plasma membrane cholesterol and thus not cause cytotoxicity and hemolytic activity, thereby facilitating intracellular metabolism and excretion of cholesterol, and effectively suppressing the secretion of IL-1β, MCP-1, and TNF-α cytokines, thereby exhibiting an excellent anti-inflammatory effect.