Improved pharmacokinetic profile of lipophilic anti-cancer drugs using ανβ3-targeted polyurethane-polyurea nanoparticles

Polyurethane-polyurea nanoparticles (PUUa NP), with redox-responsive shell and RGD peptide functionalization, were synthetized incorporating a very lipophilic chemotherapeutic drug named Plitidepsin. This system offers several clear advantages: i) good efficacy and absence of vehicle toxicity, ii) fine control of the drug stability in plasma and a controlled release inside cancer cells, iii) RGD-functionalized PUUa NP showed an excellent in vivo biodistribution, avoiding their accumulation in tissues with high presence of macrophages, and iv) PUUa NP, consequently, improved very significantly the pharmacokinetic profile of Plitidepsin, offering a very promising platform for the delivery of specially difficult and lipophilic drugs.190