Real-Time Label-Free Targeting Assessment and in Vitro Characterization of Curcumin-Loaded Poly-lactic-co-glycolic Acid Nanoparticles for Oral Colon Targeting

Mohamed A Akl, Alma Kartal-Hodzic, Teemu Suutari, Timo Oksanen, Isabella Monia Montagner, Antonio Rosato, Hatem R Ismael, Mohsen I Afouna, Paolo Caliceti, Marjo Yliperttula, Ahmed M Samy, Francesca Mastrotto, Stefano Salmaso, Tapani Viitala

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Abstract

The exploitation of curcumin for oral disease treatment is limited by its low solubility, poor bioavailability, and low stability. Surface-functionalized poly-lactic-co-glycolic acid (PLGA) nanoparticles (NPs) have shown promising results to ameliorate selective delivery of drugs to the gastro-intestinal tract. In this study, curcumin-loaded PLGA NPs (C-PLGA NPs) of about 200 nm were surface-coated with chitosan (CS) for gastro-intestinal mucosa adhesion, wheat germ agglutinin (WGA) for colon targeting or GE11 peptide for tumor colon targeting. Spectrometric and zeta potential analyses confirmed the successful functionalization of the C-PLGA NPs. Real-time label-free assessment of the cell membrane-NP interactions and NP cell uptake were performed by quartz crystal microbalance coupled with supported lipid bilayers and by surface plasmon resonance coupled with living cells. The study showed that CS-coated C-PLGA NPs interact with cells by the electrostatic mechanism, while both WGA- and GE11-coated C-PLGA NPs interact and are taken up by cells by specific active mechanisms. In vitro cell uptake studies corroborated the real-time label-free assessment by yielding a curcumin cell uptake of 7.3 ± 0.3, 13.5 ± 1.0, 27.3 ± 4.9, and 26.0 ± 1.3 μg per 104 HT-29 cells for noncoated, CS-, WGA-, and GE11-coated C-PLGA NPs, respectively. Finally, preliminary in vivo studies showed that the WGA-coated C-PLGA NPs efficiently accumulate in the colon after oral administration to healthy Balb/c mice. In summary, the WGA- and GE11-coated C-PLGA NPs displayed high potential for application as active targeted carriers for anticancer drug delivery to the colon.

Original languageEnglish
Pages (from-to)16878-16890
Number of pages13
JournalACS Omega
Volume4
Issue number16
DOIs
Publication statusPublished - Oct 15 2019

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Akl, M. A., Kartal-Hodzic, A., Suutari, T., Oksanen, T., Montagner, I. M., Rosato, A., Ismael, H. R., Afouna, M. I., Caliceti, P., Yliperttula, M., Samy, A. M., Mastrotto, F., Salmaso, S., & Viitala, T. (2019). Real-Time Label-Free Targeting Assessment and in Vitro Characterization of Curcumin-Loaded Poly-lactic-co-glycolic Acid Nanoparticles for Oral Colon Targeting. ACS Omega, 4(16), 16878-16890. https://doi.org/10.1021/acsomega.9b02086