Bioactive compounds of natural, microbial and animal origin exhibit multifunctional bioactivity against various health disorders. However, most of bioactive compounds have limited solubility, poor permeation, low stability towards GIT enzymes or follow high first pass effect. Besides this, it may exhibit non selective distribution to all organs and toxic effects on healthy cells. To subside these challenges and improve the therapeutic efficacy of bioactive compound, nanoencapsulation technique can be employed. Formulation of nanocarriers for encapsulation of bioactive molecules results in size dependent increase in aqueous solubility and permeability. Nanoencapsulation also provided stealth to harsh conditions or environment of body thereby improving the stability of bioactive compound. Nanocarriers also facilitate precise delivery of bioactive compound to target site minimizing non selective distribution to undesirable site and thus reducing undesirable side effects. Present chapter enlists the fabrication technique of bioactive compounds in nanocarriers and related benefits. The applications in bioactive compound encapsulated nanocarriers in pharmaceutical and biomedical fields was also discussed.