PMID: 9434276Jan 22, 1998Paper

The mechanism of uptake of biodegradable microparticles in Caco-2 cells is size dependent

Pharmaceutical Research
M P DesaiG L Amidon

Abstract

To study the uptake of biodegradable microparticles in Caco-2 cells. 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. 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 eff...Continue Reading

Citations

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