Nanodroplet compositions for the efficient delivery of anti-cancer agents
OwnerYang Der TIENinventor
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Abstract
Disclosed herein are nanodroplet compositions composed of a copolymer with a hydrophilic block and a hydrophobic block, a poloxamer, an oil, an anti¬cancer agent, and optionally a lyoprotectant. The nanodroplet compositions exhibit low toxicity and are biodegradable, provide for slow, sustained release of the anti-cancer agent at tumor sites, and result in a greater reduction of tumor volume when administered to subjects with cancer as compared to several commercially-available products. Furthermore, the nanodroplet compositions can be imaged and their progress through the body tracked with magnetic resonance spectroscopy or ultrasound.
Claims52
Nanodroplets comprising
- (a) a copolymer comprising a hydrophilic block and a hydrophobic block, wherein the hydrophilic block of the copolymer is polyethylene glycol or monomethoxy polyethylene glycol, and the hydrophobic block of the copolymer is polylactide, a copolymer of lactide and glycolide, a copolymer of D,L-lactide and glycolide, a polycaprolactone, a polyanhydride, or a polyorthoester;
- (b) a poloxamer,
- (c) an oil, and
- (d) an anti-cancer agent.
Nanodroplets produced by the process comprising
- (a) mixing a copolymer comprising a hydrophilic block and a hydrophobic block with an anti-cancer agent in a solvent to produce a first composition, wherein the hydrophilic block of the copolymer is polyethylene glycol or monomethoxy polyethylene glycol, and the hydrophobic block of the copolymer is polylactide, a copolymer of lactide and glycolide, a copolymer of D,L-lactide and glycolide, a polycaprolactone, a polyanhydride, or a polyorthoester;
- (b) removing the solvent from the first composition to produce a second composition;
- (c) hydrolyzing the second composition to produce a third composition;
- (d) mixing the third composition with a poloxamer and lyoprotectant to produce a fourth composition;
- (e) mixing the fourth composition with an oil to produce a fifth composition;
- and
- (f) homogenizing the fifth composition.
Dependencies are inferred from the claim text.