From Squalene to photoluminescent nanoparticles: A story

In the treatment of cancer, it is often not sufficient to find highly active molecules. The majority of active compounds have its primary target within cells and tissues and, in order to exploit the pharmacological activity, a minimum concentration is needed to be reached at the site of action. Many factors may cause a decrease in the intracellular drug concentration. Among them, low water solubility, low partition coefficient across cell membranes and extensive exportation via efflux transporters such as multi-drug resistance proteins and P-glycoproteins. For these reasons, a selective delivery of drugs to their sites of action could result in greater therapeutic effects and potentially minimize side-effects. Self-assembly drug conjugate preparation is a promising approach to improve activity and penetration through physiological barriers of potent small molecules, as well as to reduce any side effects. Drug conjugates can self-assemble in water to form nanoparticles (NPs) that offer several advantages because: (i) they are easy to obtain; (ii) they can reach high local drug concentration in tumor tissues; and (iii) they can reduce the side effects of drugs. All these factors improve drug pharmacokinetic properties.1 Based on the pioneer work of Prof. P. Couvreur in the field of nanomedicine and drug delivery and especially in the application and understanding of squalene nanoparticles, in this presentation a journey from squalene-drug nanoassemblies to tetraphenylethylene-based photoluminescent-drug nanoparticles is depicted.