Encapsulation of extremely hydrophobic substances such as SN-38 into nanoparticles, is a
promising approach to solve the solubility issue and enable drug administration. Moreover, nanocarriers’
tumor homing behavior, targeted and controlled release at the site of action will optimize therapeutic
potency and decrease toxicity of the incorporated drug substance. However, the enormous drug
hydrophobicity might limit the capacity for encapsulation as the premature drug precipitation will contribute to fast free
drug crystal growth, low drug incorporation and huge waste of the active material. In this article we defined the optimal
region for manufacturing of SN-38 loaded PEO-PPO-PEO/P(DL)LCL nanoparticles (NPs) with high efficacy of encapsulation,
suitable particle size and different surface properties, using D-optimal design and nanoprecipitation as production
method. Further we made an approach to investigate the interactions with macromolecules at the nano-bio interface which
are predetermined by the physico-chemical and surface properties of the NPs, and are important determinants for the biological
identity of the nanoparticles, the potential for evasion of the physiological barriers and the efficacy of localization
at the site of action. Here we present in depth analysis of the behavior of two types of nanoparticles with different surface
properties through structured protein interaction and bioreactivity experiments in order to presuppose NP performance and
toxicological profile in biological environment.
Keywords: D-optimal design, nano-bio interface, P(DL)LCL, PEO-PPO-PEO, Polymeric nanoparticles, protein corona, SN-38.
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