Folic acid-decorated nanocrystals as highly loaded trojan horses to target cancer cells

Marta G. Fuster, Jiawen Wang, Octavio Fandiño, Gloria Víllora, Alejandro J. Paredes*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

1 Citation (Scopus)
24 Downloads (Pure)

Abstract

The nanocrystal (NC) technology has become one of the most commonly used strategies for the formulation of poorly soluble actives. Given their large specific surface, NCs are mainly used to enhance the oral absorption of poorly soluble actives. Differently from conventional nanoparticles, which require the use of carrier materials and have limited drug loadings, NCs’ drug loading approaches 100% since they are formed of the pure drug and surrounded by a thin layer of a stabilizer. In this work, we report the covalent decoration of curcumin NCs with folic acid (FA) using EDC/NHS chemistry and explore the novel systems as highly loaded “Trojan horses” to target cancer cells. The decorated NCs demonstrated a remarkable improvement in curcumin uptake, exhibiting enhanced growth inhibition in cancer cells (HeLa and MCF7) while sparing healthy cells (J774A.1). Cellular uptake studies revealed significantly heightened entry of FA-decorated NCs into cancer cells compared to unmodified NCs while also showing reduced uptake by macrophages, indicating a potential for prolonged circulation in vivo. These findings underline the potential of NC highly loaded nanovectors for drug delivery and, in particular, for cancer therapies, effectively targeting folate receptor-overexpressing cells while evading interception by macrophages, thus preserving their viability and offering a promising avenue for precise and effective treatments.

Original languageEnglish
Pages (from-to)2781-2794
Number of pages14
JournalMolecular Pharmaceutics
Volume21
Issue number6
Early online date27 Apr 2024
DOIs
Publication statusPublished - 03 Jun 2024

Keywords

  • EDC/NHS chemistry
  • media milling
  • nanocrystals
  • nanosuspensions
  • surface decoration

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