Self-assembly nanoparticles of natural bioactive abietane diterpenes

Different approaches have been reported to enhance penetration of small drugs through physiological barriers, among them is the self-assembly drug conjugates preparation that shown to be a promising approach to improve activity and penetration, as well as to reduce any side effects. In recent years, the use of drug-conjugates, usually obtained by covalent coupling of the drug with biocompatible lipid moieties to form nanoparticles, has gained considerable attention. Natural products isolated from plants have been a successful source of potential drug leads with unique structural diversity. In the present work, three molecules derived from natural products were employed as lead molecules for the synthesis of self-assembled nanoparticles. The royleanones were conjugated with squalene, oleic acid, and/or 1-bromododecane self-assembly inducers, and conjugates were successfully synthesized and characterized. Bioactivity was assessed suggesting these nano assemblies can act as prodrugs for the release of cytotoxic lead molecules.