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

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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 , vol. 4 , no. 16 , pp. 16878-16890 . https://doi.org/10.1021/acsomega.9b02086

Title: Real-Time Label-Free Targeting Assessment and in Vitro Characterization of Curcumin-Loaded Poly-lactic-co-glycolic Acid Nanoparticles for Oral Colon Targeting
Author: Akl, Mohamed A.; Kartal-Hodzic, Alma; Suutari, Teemu; Oksanen, Timo; Montagner, Isabella Monia; Rosato, Antonio; Ismael, Hatem R.; Afouna, Mohsen I.; Caliceti, Paolo; Yliperttula, Marjo; Samy, Ahmed M.; Mastrotto, Francesca; Salmaso, Stefano; Viitala, Tapani
Contributor: University of Helsinki, Division of Pharmaceutical Biosciences
University of Helsinki, Division of Pharmaceutical Biosciences
University of Helsinki, Division of Pharmaceutical Biosciences
University of Helsinki, Drug Research Program
University of Helsinki, Division of Pharmaceutical Chemistry and Technology
Date: 2019-10-01
Language: eng
Number of pages: 13
Belongs to series: ACS Omega
ISSN: 2470-1343
URI: http://hdl.handle.net/10138/307018
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.
Subject: 317 Pharmacy
BIODEGRADABLE POLYMERIC NANOPARTICLES
SURFACE-PLASMON RESONANCE
PLGA-BASED NANOPARTICLES
DRUG-DELIVERY
CHITOSAN
LECTIN
CELLS
PERSPECTIVES
FORMULATION
ANTICANCER
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