Interaction of biodegradable nanoparticles with intestinal cells: The effect of surface hydrophilicity
Open accessAbstract
The aim of the present work was to study the influence of surface hydrophilicity of biodegradable polymeric nanoparticles on cellular uptake by Caco-2 cells. Poly(D,L-lactide-co-glycolide acid) particles loaded with a fluorescent dye, 3,3'-dioctadecyloxacarbo-cyanine perchlorate (DiO), were prepared by the emulsion-evaporation process. Three batches of particles with narrow size distribution (100, 300 and 1000 nm) were produced using selective centrifugation. One set of particles was coated by adsorption of chitosan to increase the hydrophilicity of the particles. The interaction of particles with Caco-2 cells was determined by fluorescence spectroscopy and the number of particles associated with one single cell was then calculated. Interaction with cells was clearly dependant on particle size and surface hydrophilicity. Particles in the range of 100 nm presented higher interaction when compared to larger particles. Approximately 6000 uncoated particles and more than 30,000 chitosan-coated particles were quantified per cell. Confocal microscopy confirmed the spectroscopic measurements and revealed the location of the particles in the cell monolayer. Only small particles were observed intracellularly, whereas particles larger than 300 nm were associated with the apical membranes. The location of particles <300 nm appeared to be intracellular and some particles colocalized with the nucleus.
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Surface modification with poloxamer or particle preparation with different polymers influences particle surface charge, which could contribute to reduced intestinal uptake.
“However, surface modification with poloxamer or particle preparation with different polymers influences the surface charge of the particles, which could contribute to reduced intestinal uptake [49].”
From Use of lectin-functionalized particles for oral immunotherapy (2012) · cites this paper as [49]
Gaumet et al. reported that coating PLGA particles with chitosan, which did not affect surface charge or particle size, enhanced interaction with intestinal Caco-2 cells.
“A recent study by Gaumet et al. reported that modification of surface hydrophilicity by coating PLGA particles with chitosan, which did not affect surface charge or particle size, enhanced the interaction of particles with intestinal Caco-2 cells [49].”
From Use of lectin-functionalized particles for oral immunotherapy (2012) · cites this paper as [49]
The impact of particle hydrophilicity on intestinal uptake has been described controversially in the literature.
“The impact of particle hydrophilicity on intestinal uptake has been described very controversially in literature.”
From Use of lectin-functionalized particles for oral immunotherapy (2012) · cites this paper as [49]
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Use of lectin-functionalized particles for oral immunotherapy
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- Authors
- Gaumet, M., Gurny, R., & Delie, F.
- Affiliations
- University of Geneva (CH)
- Venue
- International Journal of Pharmaceutics
- Publisher
- Elsevier BV
- Published
- 2010-05
- Volume
- 390
- Issue
- 1
- Pages
- 45-52
- ISSN
- 0378-5173 (ISSN-L)
- OpenAlex
- W2003822740
- Cited by
- 42
- References
- 25
- Citations by year
- 2026: 1 · 2025: 2 · 2022: 1 · 2021: 1 · 2018: 1 · 2017: 1 · 2016: 4 · 2015: 7 · 2014: 9 · 2013: 3 · 2012: 9
- FWCI
- 1.76
- Type
- journal article
- Language
- en
- Open access
- Licence
- Locations
- International Journal of Pharmaceutics (publishedVersion)
- PubMed (publishedVersion)
- Archive ouverte UNIGE (University of Geneva) (submittedVersion, cc-by)
- Topics
- Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Drug Solubulity and Delivery Systems
- Keywords
- biodegradable polymer nanoparticles, surface hydrophilicity, Caco-2 cells, intestinal absorption, cellular uptake, particle size, chitosan coating, PLGA, emulsion evaporation, subcellular localization, nanoparticle-cell interactions
- MeSH terms
- Polylactic Acid-Polyglycolic Acid Copolymer, Biocompatible Materials, Carbocyanines, Cell Survival, Fluorescent Dyes, Humans, Intestinal Mucosa, Microscopy, Electron, Scanning, Microscopy, Fluorescence, Particle Size, Polyglycolic Acid, Surface Properties, Microscopy, Confocal, Caco-2 Cells, Lactic Acid, Intracellular Space, Chitosan, Nanoparticles, Static Electricity
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