Theranostic polymeric nanocarriers modified by enhanced gadolinium conjugation techniques

  1. Tivadar Feczkó ORCID Logo,
  2. Albrecht Piiper,
  3. Thomas Pleli,
  4. Christian Schmithals,
  5. Dominic DenkORCID Logo,
  6. Thomas J. Vogl and
  7. Matthias G. WackerORCID Logo

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

Beilstein Arch. 2019, 20191. doi:10.3762/bxiv.2019.1.v1

Published 10 Apr 2019

  • Preprint

Abstract

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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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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© 2019 Feczkó et al.; licensee Beilstein-Institut.
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