Hydrophobic Core Carrier Compositions for Delivery of Therapeutic Agents, Methods of Making and Using the Same
First Claim
Patent Images
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, and has a molecular weight of less than about 1,000 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 about 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 about 1,000 Daltons independent of the carrier weight, andwherein each second protective 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.
0 Assignments
0 Petitions
Accused Products
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.
0 Citations
36 Claims
-
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, and has a molecular weight of less than about 1,000 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 about 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 about 1,000 Daltons independent of the carrier weight, and wherein each second protective 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, 8)
-
-
9. 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, and has a molecular weight of less than about 1,000 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 about 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 about 1,000 Daltons independent of the carrier weight, wherein each second protective 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 (10, 11, 12, 13, 14, 15, 16, 17, 18)
-
-
19. 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, and has a molecular weight of less than about 1,000 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 about 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 about 1,000 Daltons independent of the carrier weight, and wherein each second protective 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 (20, 21, 22, 23, 24, 25, 26, 27)
-
-
28. A composition, comprising
(i) a polymeric carrier; - and
(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, and has a molecular weight of less than about 1,000 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 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 to the carrier, is capable of binding a load molecule, and has a molecular weight of less than about 1,000 Daltons independent of the carrier weight; (iii) 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 about 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; (iv) a load molecule dissociably linked to the hydrophobic groups, (v) 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; (vi) optionally a targeting molecule covalently linked to the first protective side chains; and (vii) 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 (29, 30, 31, 32, 33, 34, 35, 36)
- and
Specification