Objectives: The present study aimed to enhance the aqueous solubility of methanol extract of leaves of Vinca rosea (family: Apocynaceae) by particle-size reduction using milling and to evaluate its antidiabetic activity. Materials and Methods: The methanol extract (ME) was micronized using a vibratory ball mill, operated at a vibratory speed of 15 Hz for 60 min at room temperature, and the resulting extract micronized ME (MME) was investigated to determine particle size, solubility, UV/visible profile, and in vitro antidiabetic activity. Results: The average particle size of MME was 0.753±0.227 µm, which was less than half of that of the ME (2.007±0.965 µm). The solubility of MME was greater than that of the ME. MME exhibited 65.63%, 18.0%, and 96.87% higher antidiabetic activity in the glucose uptake by the yeast cells method, hemoglobin glycosylation assay, and the alpha amylase inhibition assay, respectively (p<0.05). Conclusion: The results of the present study indicate that micronization effectively enhanced the aqueous solubility and antidiabetic activity of methanol extract of leaves of Vinca rosea.