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Real-Time Label-Free Targeting Assessment and in Vitro Characterization of Curcumin-Loaded Poly-lactic-co-glycolic Acid Nanoparticles for Oral Colon Targeting
被引:17
作者:
Akl, Mohamed A.
[1
,2
]
Kartal-Hodzic, Alma
[1
]
Suutari, Teemu
[1
]
Oksanen, Timo
[1
]
Montagner, Isabella Monia
[3
]
Rosato, Antonio
[3
,4
]
Ismael, Hatem R.
[2
]
Afouna, Mohsen, I
[2
]
Caliceti, Paolo
[5
]
Yliperttula, Marjo
[1
,5
]
Samy, Ahmed M.
[2
]
Mastrotto, Francesca
[5
]
Salmaso, Stefano
[5
]
Viitala, Tapani
[1
,6
]
机构:
[1] Univ Helsinki, Drug Res Program, Div Pharmaceut Biosci, Fac Pharm, FIN-00014 Helsinki, Finland
[2] Al Azhar Univ, Dept Pharmaceut & Ind Pharm, Fac Pharm Boys, Cairo 11884, Egypt
[3] IRCCS, Veneto Inst Oncol IOV, I-35128 Padua, Italy
[4] Univ Padua, Dept Surg Oncol & Gastroentrol, I-35131 Padua, Italy
[5] Univ Padua, Dept Pharmaceut & Pharmacol Sci, I-35131 Padua, Italy
[6] Univ Helsinki, Drug Res Program, Div Pharmaceut Chem & Technol, Fac Pharm, POB 56, FIN-00014 Helsinki, Finland
来源:
基金:
芬兰科学院;
关键词:
BIODEGRADABLE POLYMERIC NANOPARTICLES;
SURFACE-PLASMON RESONANCE;
PLGA-BASED NANOPARTICLES;
DRUG-DELIVERY;
CHITOSAN;
LECTIN;
CELLS;
PERSPECTIVES;
FORMULATION;
ANTICANCER;
D O I:
10.1021/acsomega.9b02086
中图分类号:
O6 [化学];
学科分类号:
0703 ;
摘要:
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 (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 Mayers 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 7.3 +/- 0.3, 13.5 +/- 1.0, 27.3 +/- 4.9, and 26.0 +/- 1.3 mu g per 10(4) 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.
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页码:16878 / 16890
页数:13
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