(65a) Self-Assembling Nanotechnology for Cancer Theranostics: From Computer-Assisted Design to In Vivo Applications

As a part of a pan-European task force in the field, our team has developed a series of innovative theranostic systems which proven to be excellent agents in cancer imaging and therapeutics in vivo. Specifically, exploiting the quintessence of nanotechnology, i.e., the self-assembling process of small, amphiphilic molecules, in the last decade we created a series of high-performance, non-toxic nanosized micelles that, depending on the specific chemistry, are able to (e.g.):
• encapsulate anticancer drugs with high loading capacity, enhance drug potency and combat drug resistance by promoting cellular uptake whilst decreasing drug efflux;
• perform specific and effective gene silencing via targeted small interfering RNA (siRNA) delivery;
• provide PET images with significantly superior imaging quality relating to sensitivity, specificity and accuracy when compared to the clinical standard [¹⁸F]FDG.
In this contribution we will report in details the full pathways leading to these three types of nanosystems, from their computer assisted molecular design to their in vivo performance.
References
Pricl et alì., Proc. Natl. Acad. Sci. USA, 115 (2018) 11454-11459; J. Am. Chem. Soc., 140 (2018) 16264-16274; Dagrada et al., Mol. Pharm. 15 (2018) 4689-4701; Chen et al., Small 12 (2016) 3667-3676; Wei et al., Proc. Natl. Acad. Sci. USA 112 (2015) 2978-2983; Angew. Chem. Int. Ed. Engl. 53 (2014) 11822-11827.