Cannabis sativa plants have been widely investigated for their specific compounds with medicinal properties. These bioactive compounds exert preventive and curative effects on non-communicable and infectious diseases. However, C. sativa extracts have barely been investigated, although they constitute an affordable option to treat human diseases. Nonetheless, antioxidant, antimicrobial, and immunogenicity effects have been associated with C. sativa extracts. Furthermore, innovative extraction methods in combination with nanoformulations have been proposed to increase desirable compounds’ availability, distribution, and conservation, which can be aided by modern computational tools in a transdisciplinary approach. This review aims to describe available extraction and nanoformulation methods for C. sativa, as well as its known antioxidant, antimicrobial, and immunogenic activities. Critical points on the use of C. sativa extracts in nanoformulations are identified and some prospects are envisaged.