A carbosilane dendrimer and a silacyclopentadiene analog carrying peripheral lactoses as drug-delivery systems.

Bioorg Med Chem Lett

Division of Material Science, Graduate School of Science and Technology, Saitama University, Sakura-ku, Saitama-shi, Saitama-ken, Japan.

Published: May 2012

A carbosilane dendrimer (4a) and its silacyclopentadiene analog (4b), both functionalized with lactoses, were tested for their abilities to act as drug-delivery systems. The critical micelle concentrations of 4a and 4b were measured using the drop-volume method in water and were 1.7 and 2.9 μM, respectively, suggesting that they could act as aggregates of glycoclusters. The amounts of the hydrophobic dye Orange OT loaded onto aqueous micelles of 4a and 4b and the stabilities of the dye/micelle complexes were determined by extracting the dyes from the complexes into chloroform. The particle sizes were measured for the loaded micelles by dynamic light scattering. Transfer of the dye from the micelles to peanut agglutinin was observed by fluorescence microscopy. Given the abilities of micelles of 4a and 4b to bind and release Orange OT, these glycocluster micelles may find use as drug-delivery systems.

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Source
http://dx.doi.org/10.1016/j.bmcl.2012.03.034DOI Listing

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