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April 28, 2003
Volume 81, Number 17
CENEAR 81 17 p. 10
ISSN 0009-2347


DRUG DELIVERY

MICELLES TARGET ORGANELLES

Fluorescent micelles are distributed in several cytoplasmic compartments

CELIA HENRY

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10µm      
TAKING AIM Micelles (red) target the cytoplasm rather than the nucleus (blue) or the plasma membrane (green). The pink and yellow regions show the minimal overlap.
© 2003 SCIENCE
Micelles are known to carry drugs into cells. Now, details of where block copolymer micelles might unload their cargo may speed their eventual use as drug delivery vehicles.

Pharmacology professor Dusica Maysinger, chemistry professor Adi Eisenberg, and coworkers at McGill University in Montreal use fluorescently labeled micelles made from poly(caprolactone) and poly(ethylene oxide) to determine the distribution of micelles within cells [Science, 300, 615 (2003)]. They find that these fluorescent micelles distribute themselves within several cytoplasmic compartments, including the Golgi ap- paratus and mitochondria.

"The key issue is that nothing goes into the nucleus," Maysinger says. "This is different from other micelles, which have been used specifically to target the nucleus for gene delivery."

Using a membrane-selective dye, they find that the micelles can alter the distribution of agents in a cell. By itself, the dye is confined to the plasma membrane or other membranes in the cell. But when the dye is in a micelle, it enters other cytoplasmic compartments.

"If the dye is included in the micelle, the entire cell is practically swamped with it," Maysinger says. "Much more of the dye can enter the cell when you have a nanodelivery system."

Glen S. Kwon, a pharmacy professor at the University of Wisconsin, Madison, who also studies micelles, says, "The implications are that the potency of an agent may increase and the mechanism of drug action may change in a fundamental way, owing to changes
in intracellular distribution."

Maysinger and her colleagues have started in vitro and in vivo experiments using therapeutic agents. One of the main things needed, she says, is new polymers that can provide active targeting to specific organelles.

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