pH-responsive amphiphilic block-copolymers are particularly attractive as building-block materials for self-assembled synthetic nanoplatforms (i.e. micelles, vesicles, worm-like or tubular structures). Under a slightly acidic environment (e.g. lysosomal, tumoral) the pH-sensitive block undergoes a hydrophobic to hydrophilic transition. This event translates to spontaneous dissociation of the polymeric chains and loss of the original architecture, which leads to the specific release of their cargo. Such a trait is often encountered in methacrylate-based polymeric platforms. However, despite their appealing nature, the clinical translation of methacrylates is limited as they degrade into toxic by-products.<sup> </sup>Here, we are proposing a polyester-based analogue functionalised with an imidazole moiety to introduce pH sensitivity. Upon degradation the polymer will yield only endogenous metabolites and generally recognised as safe by-products (GRAS).<br/>The proposed pH-sensitive polyester is successfully synthesised following a facile stepwise-route. Every reaction is high yielding and the final polymer has the desired molecular weight while it is also characterised by low polydispersity. The responsiveness of the polymer is proven upon self-assembly following an increase in pH. The shape and the size of the resulting morphologies are investigated by electron microscopy and light scattering techniques.<br/>The fully-metabolisable block copolymer developed here does not involve demanding synthetic protocols while it attributes pH-sensitivity to otherwise unresponsive polyesters. This makes more feasible its clinical translation for use in anticancer therapy.

Biodegradable pH-responsive polymeric nanoparticles for intracellular delivery of anticancer therapies

2019 Fall National Meeting

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