US 6,416,740 B1Granted

Acoustically active drug delivery systems

AssigneeBristol-Myers Squibb Medical Imaging, Inc.

InventorEvan C. Unger

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Abstract

The present invention is directed to targeted therapeutic delivery systems comprising a gas or gaseous precursor filled microsphere wherein said gas or gaseous precursor filled microsphere comprises an oil, a surfactant, and a therapeutic compound. Methods of preparing the targeted therapeutic delivery systems are also embodied by the present invention which comprise processing a solution comprising an oil and a surfactant in the presence of a gaseous precursor, at a temperature below the gel to liquid crystalline phase transition temperature of the surfactant to form gas or gaseous precursor filled microsphere, and adding to said microspheres a therapeutic compound resulting in a targeted therapeutic delivery system, wherein said processing is selected from the group consisting of controlled agitation, controlled drying, and a combination thereof.

Claims15

Dependent claims

A method for the controlled delivery of a therapeutic compound to a region of a patient comprising:

(i) administering to a patient a targeted therapeutic delivery system comprising, in combination with a therapeutic compound, stabilized lipid microspheres encapsulating a gas or gaseous precursor and an oil, wherein said microspheres comprises at least one phosphatidylcholine, at least one phosphatidylethanolamine, and at least one phosphatidic acid, wherein said phosphatidylcholine is selected from the group consisting of dioleoylphosphatidylcholine dimyistoylphosphatidylcholine, dipalmitoylphosphatidylcholine, and distearoyl-phosphatidylcholine;
said phosphatidylethanolamine is selected from the group consisting of dipalmitoylphosphatidylethanolamine, dipalmitoylphosphatidylethanolamine-PEG 5,000, dioleoyl-phosphatidylethanolamine, and N-succinyl-dioleoyl-phosphatidylethanolamine;
and said phosphatidic acid is dipalmatoylphosphatidic acid;
(ii) monitoring the targeted therapeutic delivery system using diagnostic ultrasound to determine the presence of the microspheres in said region;
and (iii) applying therapeutic ultrasound to said region to induce rupturing of said microspheres, thereby releasing the therapeutic compound in said region, wherein said therapeutic compound is encapsulated or embedded in said microspheres, and said therapeutic ultrasound is applied at a level below the threshold level for lethal cytotoxicity.

2 more elements

Dependencies are inferred from the claim text.

Facts

Application: 09/075,343Filed 11 May 1998 · us provisional application
Priority: 13 May 1997
Granted: 9 Jul 2002
Term ends: Not estimatedThe source records don’t support an estimate.

Classification20 codes

A61K 9/5123
Excipients; Inactive ingredients: organic compounds, e.g. fats, sugars
A61K 9/127
Dispersions; Emulsions: synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
A61K 41/0028
Medicinal preparations obtained by treating materials with wave energy or particle radiation ; Therapies using these preparations: disruption,…
A61K 47/62
The non-active ingredient being a modifying agent: the modifying agent being a protein, peptide or polyamino acid