β-Elemene is a volatile oil used for the treatment of cancer, but poor solubility, low bioavailability, and variousadversereactionslimititsapplication.Foramelioratingrisksofthevenoustoxicityofβ- elemene, intravenouslyinjectable micelle of β- elemene was prepared using the thin-film hydration method. The results pointed out the micelles were uniformly spherical with about 20.96±0.1966nm in average diameter and exhibited high entrapment efficiency (99.02％± 0.88％). As revealed by drug release studies in vitro, β- elemene micelles had sustained drug release. Compared with free β- elemene, the micelles increased the drug cellular uptake and enhanced the anti-tumor effect in vitro through retarding cell cycleandinducingapoptosis.Meanwhile,theelevatedserumstabilityofβ- elemenemicellesimpliedless drugleakageandreducedtoxicity.Thewoundhealingandtubeformationassayinvitro demonstratedthe anti-metastasis and anti-angiogenesis effects of β- elemene micelles. Moreover, the pharmacokinetics study showed the AUC and T1/2 of β- elemene in micelle group were 1.79 and 1.62 times of that in freeβ-elemene group, suggesting the circulation time of β- elemene in the blood had been prolonged. In addition, β- elemene micelles showed a favorable antitumor response compared with the β- elemene solution on C26 colon cancer-bearing mice model. Local irritation study investigated in rabbits indicated that the β- elemene micellesstrikinglymitigatedthe irritation tothe injection sitescomparedwith freeβ- elemene.Theseresults provedthatthemicellecouldbeagoodcandidateasanauspiciousdrugdelivery system of β- elemene for the prospective clinical treatment of carcinoma.