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Cited by 858Advanced Drug Delivery SystemsNanoparticle-Based Drug DeliveryDrug Solubulity and Delivery Systems

The Mechanism of Uptake of Biodegradable Microparticles in Caco-2 Cells Is Size Dependent

Desai, Manisha P., Labhasetwar, Vinod, Walter, Elke, Levy, Robert J., Amidon, Gordon L.·1997·Pharmaceutical Research
DOI 10.1023/a:1012126301290
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Abstract

Purpose To study the uptake of biodegradable microparticles in Caco-2 cells.Methods Biodegradable microparticles of polylactic polyglycolic acid co-polymer (PLGA 50:50) of mean diameters 0.1 micron, 1 micron, and 10 microns containing bovine serum albumin as a model protein and 6-coumarin as a fluorescent marker were formulated by a multiple emulsion technique. The Caco-2 cell monolayers were incubated with each diameter microparticles (100 micrograms/ml) for two hours. The microparticle uptake in Caco-2 cells was studied by confocal microscopy and also by quantitating the 6-coumarin content of the microparticles taken up by the cells. The effects of microparticle concentration, and incubation time and temperature on microparticle cell uptake were also studied.Results The study demonstrated that the Caco-2 cell microparticle uptake significantly depends upon the microparticle diameter. The 0.1 micron diameter microparticles had 2.5 fold greater uptake on the weight basis than the 1 micron and 6 fold greater than the 10 microns diameter microparticles. Similarly in terms of number the uptake of 0.1 micron diameter microparticles was 2.7 x 10(3) fold greater than the 1 micron and 6.7 x 10(6) greater than the 10 microns diameter microparticles. The efficiency of uptake of 0.1 micron diameter microparticles at 100 micrograms/ml concentration was 41% compared to 15% and 6% for the 1 micron and the 10 microns diameter microparticles, respectively. The Caco-2 cell microparticle (0.1 micron) uptake increased with concentration in the range of 100 micrograms/ml to 500 micrograms/ml which then reached a plateau at higher concentration. The uptake of microparticles increased with incubation time, reaching a steady state at two hours. The uptake was greater at an incubation temperature of 37 degrees C compared to at 4 degrees C.Conclusions The Caco-2 cell microparticle uptake was microparticle diameter, concentration, and incubation time and temperature dependent. The small diameter microparticles (0.1 micron) had significantly greater uptake compared to larger diameter microparticles. The results thus suggest that the mechanism of uptake of microparticles in Caco-2 cell is particle diameter dependent. Caco-2 cells are used as an in vitro model for gastrointestinal uptake, and therefore the results obtained in these studies could be of significant importance in optimizing the microparticle-based oral drug delivery systems.

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  • Transcytosis through the intestinal epithelial layer depends on particle size, with below 1 μm optimal for M-cell absorption, and also on particle charge and hydrophilicity.

    “The capacity of transcytosis through the intestinal epithelial layer depends on the size, with a particle size of below 1 μm for optimal M-cell absorption [30], but also on the charge and hydrophilicity of the particle carrier [31–33].”

    From Use of lectin-functionalized particles for oral immunotherapy (2012) · cites this paper as [32]

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Authors
Desai, M. P., Labhasetwar, V., Walter, E., Levy, R. J., & Amidon, G. L.
Affiliations
University of Michigan (US)
Corresponding author
Amidon, Gordon L.
ORCID
Venue
Pharmaceutical Research
Publisher
Springer Science and Business Media LLC
Published
1997-11
Volume
14
Issue
11
Pages
1568-1573
ISSN
  • 0724-8741 (ISSN-L)
  • 1573-904X
DOI
10.1023/a:1012126301290
OpenAlex
W1664986234
Cited by
858
References
33
Citations by year
2026: 5 · 2025: 22 · 2024: 20 · 2023: 16 · 2022: 38 · 2021: 22 · 2020: 43 · 2019: 34 · 2018: 25 · 2017: 42 · 2016: 46 · 2015: 41 · 2014: 59 · 2013: 45 · 2012: 62
FWCI
6.25
Type
journal article
Language
en
Open access
closed
Licence
Locations
  • Pharmaceutical Research (publishedVersion)
  • PubMed (publishedVersion)
  • Deep Blue (University of Michigan) (submittedVersion)
Topics
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
  • Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Drug Solubulity and Delivery Systems
Keywords
Caco-2 cells, biodegradable microparticles, PLGA, microparticle size, intestinal absorption, bovine serum albumin, multiple emulsions, temperature dependence, concentration dependence, incubation time, intestinal epithelial cells, drug delivery systems, oral bioavailability prediction
MeSH terms
Polylactic Acid-Polyglycolic Acid Copolymer, Animals, Cattle, Cell Membrane Permeability, Humans, Intestinal Absorption, Microspheres, Models, Biological, Particle Size, Polyglycolic Acid, Polymers, Serum Albumin, Bovine, Microscopy, Confocal, Caco-2 Cells, Lactic Acid

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