The article reviews strategies to enhance the bioavailability and therapeutic efficacy of resveratrol (RSV), a biologically active compound with antioxidant, cardioprotective, neuroprotective, anti-inflammatory, and anticancer properties. Despite its potential benefits, RSV's limited bioavailability and extensive metabolism have hindered its clinical application. The authors discuss three main approaches: combination therapies, derivatization, and encapsulation in nanoparticles. 1. **Combination Therapies**: RSV combined with established chemotherapeutic drugs has shown promising results in treating various cancers, including colon, liver, and gastric cancer. For example, RSV combined with oxaliplatin, cisplatin, 5-FU, and doxorubicin has demonstrated enhanced therapeutic effects. 2. **Derivatization**: Modifying RSV through hydroxylation, amination, methylation, prenylation, halogenation, glycosylation, and oligomerization can improve its bioavailability and biological activities. These derivatives exhibit enhanced water solubility, metabolic stability, and biological efficacy. 3. **Encapsulation in Nanoparticles**: Encapsulating RSV in different types of nanoparticles, such as polymers, metals, and lipids, can enhance its solubility, absorption, and targeted delivery. Polymer nanoparticles, metal nanoparticles, and lipid-based nanoparticles (micelles) have shown promising results in improving RSV's therapeutic outcomes. The review highlights the potential of these approaches to overcome the limitations of RSV and enhance its clinical utility.The article reviews strategies to enhance the bioavailability and therapeutic efficacy of resveratrol (RSV), a biologically active compound with antioxidant, cardioprotective, neuroprotective, anti-inflammatory, and anticancer properties. Despite its potential benefits, RSV's limited bioavailability and extensive metabolism have hindered its clinical application. The authors discuss three main approaches: combination therapies, derivatization, and encapsulation in nanoparticles. 1. **Combination Therapies**: RSV combined with established chemotherapeutic drugs has shown promising results in treating various cancers, including colon, liver, and gastric cancer. For example, RSV combined with oxaliplatin, cisplatin, 5-FU, and doxorubicin has demonstrated enhanced therapeutic effects. 2. **Derivatization**: Modifying RSV through hydroxylation, amination, methylation, prenylation, halogenation, glycosylation, and oligomerization can improve its bioavailability and biological activities. These derivatives exhibit enhanced water solubility, metabolic stability, and biological efficacy. 3. **Encapsulation in Nanoparticles**: Encapsulating RSV in different types of nanoparticles, such as polymers, metals, and lipids, can enhance its solubility, absorption, and targeted delivery. Polymer nanoparticles, metal nanoparticles, and lipid-based nanoparticles (micelles) have shown promising results in improving RSV's therapeutic outcomes. The review highlights the potential of these approaches to overcome the limitations of RSV and enhance its clinical utility.