Theranostic polymeric nanocarriers modified by enhanced gadolinium conjugation techniques

Submitting author affiliation:
Hungarian Academy of Sciences Research Centre for Natural Sciences, Budapest, Hungary

Beilstein Arch. 2019, 20191.

Published 10 Apr 2019

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This preprint has not been peer-reviewed. When a peer-reviewed version is available, this information will be updated.


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.

Keywords: gadolinium; drug release; polymeric nanocarrier; sorafenib; theranostic nanoparticles

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When a peer-reviewed version of this preprint is available, this information will be updated in the information box above. If no peer-reviewed version is available, please cite this preprint using the following information:

Feczkó, T.; Piiper, A.; Pleli, T.; Schmithals, C.; Denk, D.; Vogl, T. J.; Wacker, M. G. Beilstein Arch. 2019, 20191. doi:10.3762/bxiv.2019.1.v1

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