TY - JOUR A1 - Feczkó, Tivadar A1 - Piiper, Albrecht A1 - Pleli, Thomas A1 - Schmithals, Christian A1 - Denk, Dominic A1 - Vogl, Thomas J. A1 - Wacker, Matthias G. T1 - Theranostic polymeric nanocarriers modified by enhanced gadolinium conjugation techniques JF - Beilstein Archives Y1 - 2019/// SN - M3 - doi:10.3762/bxiv.2019.1.v1 N2 - Background: Efficient delivery of the poorly water-soluble compound sorafenib still poses a challenge to current formulation strategies. To incorporate the lipophilic molecule into biocompatible and biodegradable theranostic nanoparticles has great potential for improving efficacy and safety of cancer therapy.Results: In this study, sorafenib nanoencapsulation was optimized using poly(D,L-lactide-co-glycolide) and polyethylene glycol-poly(D,L-lactide-co-glycolide) copolymers comparing three different technologies. The particles ranged in size between 220 and 240 nm with encapsulation efficiencies from 76.1 ± 1.7 % to 69.1 ± 10.1 %. A remarkable maximum drug load of 9.0 % was achieved. Finally, a gadolinium complex was covalently attached to the nanoparticle surface transforming the nanospheres into theranostic devices allowing the localization using magnetic resonance imaging.Conclusion: The manufacture of sorafenib-loaded nanoparticles and the functionalization of the particle surface with a gadolinium complex resulted in a high drug loading, a strong MRI signal, optimal stability features and a sustained release profile. ER -