Breast cancer is one of the main causes of death in women. Uncaria gambir is an Indonesian herbal plant that can be used as an anti-cancer. However, herbal medicines have low bioavailability, which affects their bioactivity. Nanoencapsulation can increase bioavailability and stability of bioactive compounds in herbal medicines.This recent finding tried to unravel anti-cancer and chemopreventive of U. gambir nano-encapsulated by Na-alginate.U. gambir bioactive compounds were isolated and characterized using UV-Vis spectrometer, FTIR, NMR and HR-MS. U. gambir extract was nanoencapsulated using Na-alginate. Anti-cancer effect was assessed by MTT assay towards T47D cell. Meanwhile, a chemopreventive analysis was carried out in breast cancer mice-induced benzo[α]pyrene. The healthy mice were divided into 8 groups comprising control and treatment.Elucidation of U. gambir ethyl acetate extract confirmed high catechin content, 89.34% (w/w). Successful nanoencapsulation of U. gambir (G-NPs) was indicated. The particle size of G-NPs was 78.40 ± 12.25 nm. Loading efficiency (LE) and loading amount (LA) of G-NPs were 97.56 ± 0.04% and 32.52 ± 0.01%, respectively. G-NPs had an EC50 value of 10.39 ± 3.50 µg/mL, which was more toxic than the EC50 value of extract towards the T47D cell line. Administration of 200 mg/kg BW G-NPs to mice induced by benzo[α]pyrene exhibited SOD and GSH levels of 13.69 ng/mL and 455.6 ng/mL. In addition, the lowest TNF-α level was 27.96 ng/mL. A dose of 100 mg/kg BW G-NPs could best increase CAT levels by 7.18 ng/mL. There was no damage or histological abnormalities found in histological analysis of the breast tissue in the group given 200 mg/kg BW G-NPs.