Cross-linkable phosphonate-containing supramolecular complexes and their use for delivery of therapeutic and diagnostic agents
OwnerCatherine J. Page, Marcus Helfrichinventors
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Abstract
Cross-linkable, phosphonate containing supramoleuclar aggregates are disclosed, which may be used to advantage, for example, as drug delivery vehicles for the treatment of bone-related disorders.
Claims30
A composition which comprises a therapeutic or diagnostic agent and stabilized supramolecular aggregates comprising a phosphonate or a combination of chemically distinct phosphonates, said phosphonate(s) having hydrophillic head groups, and hydrophobic tail groups comprising a straight or branched hydrocarbon chain, at least a portion of said hydrophobic tail groups having at least one cross-linkable moiety, said aggregates having a polar exterior region comprising said hydrophillic head groups and a non-polar core region comprising said hydrophobic tail groups, said supramolecular aggregates being stabilized by cross-links formed between the cross-linkable moieties of said hydrophobic tail groups.
A method of making supramolecular aggregates comprising a phosphonate or a combination of chemically distinct phosphonates, said phosphonate(s), having hydrophilic head groups and hydrophobic tail groups comprising a straight or branched hydrocarbon chain, at least a portion of said hydrophobic tail groups having at least one cross-linkable moiety, said aggregates having a polar exterior region comprising said hydrophilic head groups and a non-polar core region comprising said hydrophobic tail groups, said method comprising:
- a. mixing a predetermined quantity of said phosphonate(s) with a sufficient amount of a biologically acceptable buffer to form a mixture, heating said mixture to boiling, and cooling said mixture, thereby providing an array of aggregates of diverse size;
- b. subjecting the resulting mixture to extrusion to produce supramolecular aggregates of uniform size distribution;
- and
- c. irradiating said aggregate with a light source generating energy effective to form cross-links between the cross-linkable moieties of said hydrophobic tail groups.
Dependencies are inferred from the claim text.