There is limited information on how postharvest drying of Artemisia annua affects artemisinin (ART) biosynthesis and A. annua antioxidant capacity. Antioxidants may boost the bioactivity of ART and the crop commercial value. We evaluated the effect of freeze, oven, shade, and sun drying, time of drying, and light intensity on the leaf concentration of ART, dihydroartemisinic acid (DHAA), artemisinic acid (AA), and on the leaf antioxidant capacity. Freeze-dried samples had the lowest ART concentrations as compared to the other drying methods. However, the ferric reducing antioxidant power assay showed that freeze- and oven-dried samples had similarly high antioxidant activities, which declined significantly after plants were shade- and sun-dried. Shade drying for 1, 2, and 3 weeks, under ambient or low light, did not change the ART content but significantly decreased the leaf antioxidant activity, mainly if sun-dried. A significant decrease (82% average) in DHAA was observed for all drying procedures as compared to freeze drying, with a simultaneous, significant increase in ART (33% average). The average bioconversion of DHAA to ART was 43% for oven- and shade-dried plants and 94% for sun-dried plants, reiterating the hypothesis that DHAA, not AA, is the main biosynthetic precursor of ART and suggesting that sun drying improves the bioconversion from DHAA to ART. Data also indicate that oven drying for 24 h at 45 degrees C can provide good levels of both ART and antioxidants in leaves. These findings are valuable for the commercial production of ART and of bioactive antioxidants that might synergize with the antimalarial and anticancer effects of ART when combined in traditional preparations to improve human and animal health.