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

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 gastrointestinal tract. In this study, curcumin-loaded PLGA NPs (CPLGA 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 CPLGA 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.

Publication year: 2019
Authors: 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,⊥ and Tapani Viitala*,†,#

†Drug Research Program, Division of Pharmaceutical Biosciences, Faculty of Pharmacy, University of Helsinki, 00014 Helsinki, Finland
‡Department of Pharmaceutics and Ind. Pharmacy, Faculty of Pharmacy (Boys), Al-Azhar University, Nasr City, 11884 Cairo, Egypt
§Veneto Institute of Oncology IOV-IRCCS, 35128 Padua, Italy
∥Department of Surgery, Oncology and Gastroentrology and ⊥Department of Pharmaceutical and Pharmacological Sciences, University of Padova, 35131 Padova, Italy

Published in: ASC Omega
DOI: 10.1021/acsomega.9b02086


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