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Gold nanoparticle conjugates with a pH-sensitive ligand for chemo- and radiotherapy applications
Type: Patent. Reference code: 200805R-Romero, F
Holding entities
  • Universitat de València
  • Catalan Institute of Nanoscience and Nanotechnology
  • University of Santiago de Compostela
  • Catalan Institution for Research and Advanced Studies
UV inventor staff
  • Romero Martinez, Francisco Manuel
  • PDI-Titular d'Universitat
  • Director/a de Departament
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Non-UV inventor staff
  • Óscar Gallego Rubio
  • Víctor Franco Puntes
  • Fernando Domínguez Puente
Background

Platinum compounds play an important role in chemotherapy treatments. Cisplatin, the first generation of platinum-based chemotherapeutic drugs, is one of the most common anticancer agents, having a broad spectrum of anticancer activity. However, despite its efficacy, the use of cisplatin has disadvantages such as high toxicity due to its poor selectivity between malignant and benign cells (leading to neurotoxicity, neurotoxicity and ototoxicity), or the development of intrinsic or acquired resistance during treatment. Although significant efforts have been made to address these problems through the development of new generations of platinum derivatives, improvements have not been significant. Thus, second generation platinum-based drugs such as carboplatin or oxyplatin have less renal and gastrointestinal toxicity, but show bone marrow toxicity, and have less anticancer potential than cisplatin, with limited efficacy and spectrum of action.

Invention

The research group has successfully synthesised AuNP-CisPt conjugates in aqueous solution, stable under physiological conditions. Upon contact with cells, the CisPt-conjugated nanoparticles are passively endocytosed, accumulating in the tumour like other antineoplastic drugs. Once in the endosome, the drop in pH releases CisPt, which can migrate freely to the nucleus and cause cell death. Cytotoxicity studies suggest that CisPt is more toxic when transported into cells by AuNPs than in its native form. Thus, the first step in the design of a new drug delivery system has been proven.

Applications

In the pharmaceutical industry, for the development of new cancer treatments using gold nanoparticles for the release of high doses of cisplatin chemotherapeutic agents.

Competitive advantages

The main benefits of the invention are:

  • High drug release capacity, as the new invention allows 10 times more platinum to be released into the tumour than by alternative methods.
  • Reduction of side effects on healthy tissues, such as toxicity.
  • Reduced tumour resistance to platinum compounds.
Intellectual property status
  • Patent granted
Contact
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