Nanodroplet compositions for the efficient delivery of anti-cancer agents
OwnerDer-Yang 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.
Claims24
One or more nanodroplets, each nanodroplet comprising
- (a) a copolymer comprising a hydrophilic block and a hydrophobic block, wherein the hydrophilic block of the copolymer is monomethoxy polyethylene glycol having a molecular weight from 1,500 Da to 2,500 Da and the hydrophobic block of the copolymer is poly(D,L-lactide) having a molecular weight from 1,500 Da to 2,500 Da;
- (b) a poloxamer having the formula
- HO(C2H4O)b(C3H6O)a(C2H4O)bH
- wherein a is from 25 to 35 and b is from 70 to 80,
- (c) a hydrophobic core comprising an oil comprising a mixture of caprylic triglyceride and capric triglyceride,
- (d) an anti-cancer agent, and
- (e) a lyoprotectant,
- wherein
- the dry weight ratio of anti-cancer agent to the copolymer is from 1:5 to 1:9,
- the dry weight ratio of anti-cancer agent to the poloxamer is from 1:3 to 1:5,
- the weight ratio of oil to the copolymer is from 0.1 to 1,
- the dry weight ratio of lyoprotectant to the copolymer is from 0.1 to 1, and
- the nanodroplets have a Z-average diameter from 100 nm to 150 nm.
Dependencies are inferred from the claim text.