Liposome formulations of boronic acid compounds
First Claim
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1. A composition, comprising liposomes formed of a vesicle-forming lipid, and entrapped in said liposomes, a boronate ester compound prepared from a peptide boronic acid compound and a polyol, with the proviso that the peptide boronic acid compound is not bortezomib.
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Abstract
A liposome composition comprised of liposomes having a peptide boronic acid proteasome inhibitor compound entrapped in the liposomes is described. The boronic acid compound is entrapped in the liposomes in the form of a boronate ester, subsequent to interaction with a liposome-entrapped polyol. In one embodiment, the liposomes have an outer coating of hydrophilic polymer chains and are used to treat a malignancy in a subject.
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Citations
23 Claims
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1. A composition, comprising
liposomes formed of a vesicle-forming lipid, and entrapped in said liposomes, a boronate ester compound prepared from a peptide boronic acid compound and a polyol, with the proviso that the peptide boronic acid compound is not bortezomib.
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17. A treatment method, comprising
preparing liposomes having in entrapped form a boronate ester compound prepared from a peptide boronic acid compound and a polyol, and; administering the liposomes to a subject. - View Dependent Claims (18, 19, 20)
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21. A method of selectively destroying tumor tissue in a tumor-bearing subject undergoing radiation therapy, comprising
administering to a tumor-bearing subject, liposomes having in entrapped from (i) a boronate ester compound prepared from a peptide boronic acid compound and a polyol and (ii) an isotope of boron; - and
subjecting said subject to radiation therapy. - View Dependent Claims (22, 23)
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Specification