Boron-Containing Lipids and Liposomes: New Conjugates of Cholesterol with Polyhedral Boron Hydrides

Chemistry : a European Journal
Vladimir I BregadzeNarayan S Hosmane

Abstract

A series of boron-containing lipids were prepared by reactions of cyclic oxonium derivatives of polyhedron boranes and metallacarboranes ( closo- dodecaborate anion, cobalt and iron bis(dicarbollides)) with amine and carboxylic acids which are derived from cholesterol. Stable liposomal formulations, on the basis of synthesized boron-containing lipids, HSPC and DSPE-PEG as excipients, were prepared and then characterized by dynamic light scattering (DLS) that revealed the formation of particles to be smaller than 200 nm in diameter. The resulting liposomal formulations showed moderate to excellent loading and entrapment efficiency, thus justifying the design of the compounds to fit in the lipid bilayer and ensuring ease of in vivo use for future application. The liposome formulations based on cobalt and iron bis(dicarbollide)-based lipids were found to be non-toxic against both human breast normal epithelial cells MCF-10A and human breast cancer cells MCF-7.

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Citations

Dec 20, 2020·Journal of Pharmaceutical Sciences·Ravindra Dhar DubeyNarayan S Hosmane
Jan 28, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Anna A DruzinaVladimir I Bregadze
Jan 29, 2021·ChemMedChem·Marta GozziEvamarie Hey-Hawkins
Nov 30, 2021·Langmuir : the ACS Journal of Surfaces and Colloids·Nicholas A BernierAlexander M Spokoyny

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