In order to improve the stability of α-tocopherol (α-TOC) under natural environment and enhance its encapsulation rate and drug utilization, β-cyclodextrin derivative (β-CD-6-DA) modified by dopamine was used as host molecule to self-embed α-TOC, thereby obtaining stable inclusion complex (β-CD-6-DA/α-TOC). The encapsulation rate, molecular recognition behaviors and inclusion proportion of β-CD-6-DA on α-TOC were investigated using UV-vis, 2D-NOESY, and continuous variable Job’s methods, which exhibited up to 99.3±0.7% of encapsulation efficiency, promoted embedded depth of α-TOC inside hydrophobic cavity, and increased inclusion proportion from 2 : 1 to 1 : 1. Furthermore, the biological properties of β-CD-6-DA/α-TOC inclusion complex were discussed, revealing excellent cytocompatibility, controlled release at 35 ℃, and enhanced anti-oxidative scavenging capacity.