The design of nanocarriers that selectively target the liver or kidney is a significant challenge in drug delivery due to the diverse physiological structures and inherent characteristics, as well as their distinct requirements for nanocarriers. Herein, a strategy to synthesize a series of second near‐infrared region (NIR‐II) emitting gold nanocarriers for fine‐tuning liver or kidney‐specific delivery via altering their surface chemistry using cucurbit[7]uril (CB[7]) and Cys‐Arg‐Gly‐Asp (CRGD) peptide is reported. Accordingly, it shows that ultrasmall nanocarriers can facilitate kidney‐targeted delivery in cisplatin‐induced acute kidney injury (AKI) mice, which significantly boosted the accumulation of dexamethasone (DXM) loaded onto the nanocarriers at the site of injured kidneys, thereby achieving improved therapeutic results. Thus, this organ‐specific delivery strategy holds tremendous promise for improving drug delivery efficiency and providing new perspectives and methods for personalized treatments.