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Last Updated: January 26, 2020

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Claims for Patent: 8,697,031

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Summary for Patent: 8,697,031
Title:Dual function polymer micelles
Abstract: The invention relates to micelles that are elaborated with functionality useful for imaging and/or selectively targeting tissue, e.g., in the delivery of hydrophobic agents.
Inventor(s): Ai; Hua (Sichuan, CN), Duerk; Jeffrey L. (Avon Lake, OH), Flask; Chris (Avon Lake, OH), Gao; Jinming (Plano, TX), Lewin; Jonathan S. (Baltimore, MD), Shuai; Xintao (Cleveland Heights, OH), Weinberg; Brent (Cleveland Heights, OH)
Assignee: Case Western Reserve University (Cleveland, OH)
Application Number:11/569,989
Patent Claims:1. A micellar structure comprising a biocompatible amphiphilic block copolymer selected from PBLG-PEO, PEO-PPO-PEO, PEG-b-PBLA, and PCL-PEG, a hydrophobic chemotherapeutic agent encapsulated within the micellar structure, a functionalized corona comprising a tissue- or tumor-specific targeting peptide sequence, and an imaging agent comprising an MRI contrast agent encapsulated within the micellar structure, the MRI contrast agent comprising superparamagnetic iron oxide, wherein the tissue-specific targeting peptide sequence and the tumor-specific targeting peptide sequence is selected from SEQ ID Nos 1-756.

2. A micellar structure of claim 1, wherein the amphiphilic copolymer is PCL-PEG.

3. A micellar structure of claim 1, wherein the chemotherapeutic agent is selected from aminoglutethimide, amsacrine, anastrozole, asparaginase, bcg, bicalutamide, bleomycin, buserelin, busulfan, campothecin, capecitabine, carboplatin, carmustine, chlorambucil, cisplatin, cladribine, clodronate, colchicine, cyclophosphamide, cyproterone, cytarabine, dacarbazine, dactinomycin, daunorubicin, dienestrol, diethylstilbestrol, docetaxel, doxorubicin, epirubicin, estradiol, estramustine, etoposide, exemestane, filgrastim, fludarabine, fludrocortisone, fluorouracil, fluoxymesterone, flutamide, gemcitabine, genistein, goserelin, hydroxyurea, idarubicin, ifosfamide, imatinib, interferon, irinotecan, ironotecan, letrozole, leucovorin, leuprolide, levamisole, lomustine, mechlorethamine, medroxyprogesterone, megestrol, melphalan, mercaptopurine, mesna, methotrexate, mitomycin, mitotane, mitoxantrone, nilutamide, nocodazole, octreotide, oxaliplatin, paclitaxel, pamidronate, pentostatin, plicamycin, porfimer, procarbazine, raltitrexed, rituximab, streptozocin, suramin, tamoxifen, temozolomide, teniposide, testosterone, thioguanine, thiotepa, titanocene dichloride, topotecan, trastuzumab, tretinoin, vinblastine, vincristine, vindesine, and vinorelbine.

4. A micellar structure of claim 3, wherein the chemotherapeutic agent is selected from paclitaxel and doxorubicin.

5. A micellar structure of claim 1, wherein the peptide sequence is a .alpha..sub.v.beta..sub.3 ligand.

6. A micellar structure of claim 5, wherein the .alpha..sub.v.beta..sub.3 ligand is cRGD.

7. A micellar structure of claim 1, wherein the functionalized corona comprises a second imaging agent.

8. A micellar structure of claim 7, wherein the second imaging agent comprises a chelating agent.

9. A micellar structure of claim 8, wherein the chelating agent is selected from DOTA, DTPA-BMA, DTPA-BP, and CDTA.

10. A micellar structure of claim 8, further comprising a radioactive moiety that is chelated by the chelating agent.

11. A micellar structure of claim 10, wherein the radioactive moiety is selected from .sup.225Ac, .sup.227Ac, .sup.241Am, .sup.198Au, .sup.7Be, .sup.212Bi, .sup.48Ca, .sup.109Cd, .sup.139Ce, .sup.141Ce, .sup.252Cf, .sup.55Co, .sup.57Co, .sup.60Co, .sup.51Cr, .sup.130Cs, .sup.131Cs, .sup.137Cs, .sup.61Cu, .sup.62Cu, .sup.165Dy, .sup.152Eu, .sup.155Eu, .sup.18F, .sup.55Fe, .sup.59Fe, .sup.64Ga, .sup.67Ga, .sup.68Ga, .sup.153Gd, .sup.68Ge, .sup.111In, .sup.115mIn, .sup.191mIr, .sup.192Ir, .sup.177Lu, .sup.51Mn, .sup.52Mn, .sup.99Mo, .sup.95Nb, .sup.194Os, .sup.203Pb, .sup.212Pb, .sup.103Pd, .sup.109Pd, .sup.238Pu, .sup.223Ra, .sup.226Ra, .sup.82Rb, .sup.186Re, .sup.188Re, .sup.105Rh, .sup.97Ru, .sup.103Ru, .sup.145Sm, .sup.153Sm, .sup.117mSn, .sup.85Sr, .sup.89Sr, .sup.90Sr, .sup.178Ta, .sup.179Ta, .sup.182Ta, .sup.149Tb, .sup.96Tc, .sup.99mTc, .sup.228Th, .sup.229Th, .sup.201Tl, .sup.170Tm, .sup.171Tm, .sup.188W, .sup.88Y, .sup.90Y, .sup.91Y, .sup.169Yb, .sup.62Zn, .sup.65Zn, .sup.99mTc-labeled Annexin V.sup.28, and .sup.95Zr.

12. A micellar structure of claim 11, wherein the radioactive moiety is selected from .sup.99mTc-labeled Annexin V.sup.28, and .sup.111In.

13. A pharmaceutical composition comprising micelles of claim 1 and a pharmaceutically acceptable carrier.

Summary for Patent:   Start Trial

PCT Information
PCT FiledJune 02, 2005PCT Application Number:PCT/US2005/019308
PCT Publication Date:December 22, 2005PCT Publication Number:WO2005/120585

Details for Patent 8,697,031

Applicant Tradename Biologic Ingredient Dosage Form BLA Number Approval Date Patent No. Assignee Estimated Patent Expiration Status Orphan Source
Merck ELSPAR asparaginase VIAL 101063 001 1978-01-10   Start Trial Case Western Reserve University (Cleveland, OH) 2024-06-06 RX search
Amgen NEUPOGEN filgrastim VIAL 103353 001 1991-02-20   Start Trial Case Western Reserve University (Cleveland, OH) 2024-06-06 RX search
Amgen NEUPOGEN filgrastim VIAL 103353 002 1991-02-20   Start Trial Case Western Reserve University (Cleveland, OH) 2024-06-06 RX search
Amgen NEUPOGEN filgrastim SYRINGE 103353 003 1991-02-20   Start Trial Case Western Reserve University (Cleveland, OH) 2024-06-06 RX search
Amgen NEUPOGEN filgrastim SYRINGE 103353 004 1991-02-20   Start Trial Case Western Reserve University (Cleveland, OH) 2024-06-06 RX search
Genentech RITUXAN rituximab VIAL 103705 001 1997-11-26   Start Trial Case Western Reserve University (Cleveland, OH) 2024-06-06 RX Orphan search
>Applicant >Tradename >Biologic Ingredient >Dosage Form >BLA >Number >Approval Date >Patent No. >Assignee >Estimated Patent Expiration >Status >Orphan >Source

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