Hydrophobic core carrier compositions for delivery of therapeutic agents, methods of making and using the same
First Claim
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1. A composition, consisting of:
- (i) a polymeric carrier;
(ii) a plurality of first hydrophobic groups, wherein each first hydrophobic group of the plurality of first hydrophobic groups is covalently linked to the carrier, is capable of binding a load molecule, comprises an alkyl group of 8-36 carbons, and has a molecular weight between 150 to 1000 Daltons independent of the carrier weight;
(iii) a plurality of first protective side chains, wherein each first protective side chain is covalently linked to the carrier and has a molecular weight between about 400 and 20,000 Daltons independent of the carrier weight, and wherein each first protective side chain is polyethylene glycol, polypropylene glycol, a co-polymer of polyethylene glycol and polypropylene glycol, or an alkoxy derivative thereof;
(iv) optionally a plurality of second hydrophobic groups, wherein each second hydrophobic group is covalently linked at a first end to the carrier and is linked at a second end to a second protective side chain having a molecular weight between 400 and 20,000 Daltons independent of the carrier weight,wherein each second hydrophobic group is capable of binding a load molecule, has a molecular weight of less than 1,000 Daltons independent of the carrier weight, andwherein each second protective side chain is polyethylene glycol, polypropylene glycol, a co-polymer of polyethylene glycol and polypropylene glycol, or an alkoxy derivative thereof; and
(v) a load molecule dissociably linked to the hydrophobic groups; and
(vi) a pharmaceutically acceptable excipient;
wherein a weight ratio of total protective side chains to total hydrophobic groups is more than 17;
1 and the composition is soluble in aqueous buffer.
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Abstract
The present invention relates, in part, to a biocompatible hydrophobic-core carrier comprising a carrier, and a plurality of hydrophobic groups covalently linked to the polymeric carrier. The hydrophobic groups are capable of dissociably linking load molecules such as therapeutic agents. The hydrophobic-core carrier may also comprise protective side chains, orienting molecules, and targeting molecules.
108 Citations
32 Claims
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1. A composition, consisting of:
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(i) a polymeric carrier; (ii) a plurality of first hydrophobic groups, wherein each first hydrophobic group of the plurality of first hydrophobic groups is covalently linked to the carrier, is capable of binding a load molecule, comprises an alkyl group of 8-36 carbons, and has a molecular weight between 150 to 1000 Daltons independent of the carrier weight; (iii) a plurality of first protective side chains, wherein each first protective side chain is covalently linked to the carrier and has a molecular weight between about 400 and 20,000 Daltons independent of the carrier weight, and wherein each first protective side chain is polyethylene glycol, polypropylene glycol, a co-polymer of polyethylene glycol and polypropylene glycol, or an alkoxy derivative thereof; (iv) optionally a plurality of second hydrophobic groups, wherein each second hydrophobic group is covalently linked at a first end to the carrier and is linked at a second end to a second protective side chain having a molecular weight between 400 and 20,000 Daltons independent of the carrier weight, wherein each second hydrophobic group is capable of binding a load molecule, has a molecular weight of less than 1,000 Daltons independent of the carrier weight, and wherein each second protective side chain is polyethylene glycol, polypropylene glycol, a co-polymer of polyethylene glycol and polypropylene glycol, or an alkoxy derivative thereof; and (v) a load molecule dissociably linked to the hydrophobic groups; and (vi) a pharmaceutically acceptable excipient; wherein a weight ratio of total protective side chains to total hydrophobic groups is more than 17;
1 and the composition is soluble in aqueous buffer. - View Dependent Claims (2, 3, 4, 5, 6, 7)
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8. A composition, consisting of:
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(i) a polymeric carrier; (ii) a plurality of first hydrophobic groups, wherein each first hydrophobic group of the plurality of first hydrophobic groups is covalently linked to the carrier, is capable of binding a load molecule, comprises an alkyl group of 8-36 carbons, and has a molecular weight between 150 to 1000 Daltons independent of the carrier weight; (iii) a plurality of first protective side chains, wherein each first protective side chain is covalently linked to the carrier and has a molecular weight between about 400 and 20,000 Daltons independent of the carrier weight, and wherein each first protective side chain is polyethylene glycol, polypropylene glycol, a co-polymer of polyethylene glycol and polypropylene glycol, or an alkoxy derivative thereof; (iv) optionally a plurality of second hydrophobic groups, wherein each second hydrophobic group is covalently linked at a first end to the carrier and is linked at a second end to a second protective side chain having a molecular weight between 400 and 20,000 Daltons independent of the carrier weight, wherein each second hydrophobic group is capable of binding a load molecule, has a molecular weight of less than 1,000 Daltons independent of the carrier weight, wherein each second protective side chain is polyethylene glycol, polypropylene glycol, a co-polymer of polyethylene glycol and polypropylene glycol, or an alkoxy derivative thereof; (v) a load molecule dissociably linked to the hydrophobic groups; (vi) an orienting molecule covalently linked to the carrier, wherein the orienting molecule is selected from the group consisting of sulfate, sulfonate, phosphate, phosphonate, bisphosphonate, lysine, and arginine; (vii) optionally a targeting molecule covalently linked to the first protective side chains; and (viii) a pharmaceutically acceptable excipient; wherein a weight ratio of total protective side chains to total hydrophobic groups is more than 17;
1 and the composition is soluble in aqueous buffer. - View Dependent Claims (9, 10, 11, 12, 13, 14, 15, 16)
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17. A composition, consisting of:
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(i) a polymeric carrier; (ii) a plurality of first hydrophobic groups, wherein each first hydrophobic group of the plurality of first hydrophobic groups is covalently linked to the carrier, is capable of binding a load molecule, comprises an alkyl group of 8-36 carbons, and has a molecular weight between 150 to 1000 Daltons independent of the carrier weight; (iii) a plurality of first protective side chains, wherein each first protective side chain is covalently linked to the carrier and has a molecular weight between and 20,000 Daltons independent of the carrier weight, and wherein each first protective side chain is polyethylene glycol, polypropylene glycol, a co-polymer of polyethylene glycol and polypropylene glycol, or an alkoxy derivative thereof; (iv) optionally a plurality of second hydrophobic groups, wherein each second hydrophobic group is covalently linked at a first end to the carrier, and is linked at a second end to a second protective side chain having a molecular weight between 400 and 20,000 Daltons independent of the carrier weight, wherein each second hydrophobic group is capable of binding a load molecule, has a molecular weight of less than 1,000 Daltons independent of the carrier weight, and wherein each second protective side chain is polyethylene glycol, polypropylene glycol, a co-polymer of polyethylene glycol and polypropylene glycol, or an alkoxy derivative thereof; (v) a load molecule dissociably linked to the hydrophobic groups; (vi) a targeting molecule covalently linked to the first protective side chains; and (vii) a pharmaceutically acceptable excipient; wherein a weight ratio of total protective side chains to total hydrophobic groups is more than 17;
1 and the composition is soluble in aqueous buffer. - View Dependent Claims (18, 19, 20, 21, 22, 23, 24)
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25. A composition, comprising:
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(i) a polymeric carrier; (ii) a plurality of first hydrophobic groups, wherein each first hydrophobic group of the plurality of first hydrophobic groups is covalently linked at a first end to the carrier, is capable of binding a load molecule, comprises an alkyl group of 8-36 carbons, and has a molecular weight between 150 to 1000 Daltons independent of the carrier weight; (iii) a plurality of first protective side chains, wherein each first protective side chain is covalently linked to a second end of the first hydrophobic group, and has a molecular weight between 400 and 20,000 Daltons independent of the carrier weight, and wherein each first protective side chain is polyethylene glycol, polypropylene glycol, a co-polymer of polyethylene glycol and polypropylene glycol, or an alkoxy derivative thereof; (iv) optionally a plurality of second hydrophobic groups, wherein each second hydrophobic group is covalently linked to the carrier, is capable of binding a load molecule, and has a molecular weight of less than 1,000 Daltons independent of the carrier weight; (v) optionally a plurality of second protective side chains, wherein each second protective side chain is covalently linked to the carrier and has a molecular weight between 400 and 20,000 Daltons independent of the carrier weight, and wherein each second protective side chain is polyethylene glycol, polypropylene glycol, a co-polymer of polyethylene glycol and polypropylene glycol, or an alkoxy derivative thereof; (vi) a load molecule dissociably linked to the hydrophobic groups; (vii) optionally an orienting molecule covalently linked to the carrier, wherein the orienting molecule is selected from the group consisting of sulfate, sulfonate, phosphate, phosphonate, bisphosphonate, lysine, and arginine; (viii) optionally a targeting molecule covalently linked to the first protective side chains; and (ix) a pharmaceutically acceptable excipient; wherein the weight ratio of the total protective side chains to the total hydrophobic groups is more than 17;
1 and the composition is soluble in aqueous buffer. - View Dependent Claims (26, 27, 28, 29, 30, 31, 32)
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Specification