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Last Updated: March 29, 2024

Claims for Patent: 7,638,558


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Summary for Patent: 7,638,558
Title:Polymeric micelles for drug delivery
Abstract: The present invention relates to the field of polymer chemistry and more particularly to multiblock copolymers and micelles comprising the same.
Inventor(s): Breitenkamp; Kurt (Northampton, MA), Sill; Kevin N. (Tampa, FL), Skaff; Habib (Tampa, FL), Breitenkamp; Rebecca (Northampton, MA)
Assignee: Intezyne Technologies, Inc. (Tampa, FL)
Application Number:11/396,872
Patent Claims:1. A drug-loaded micelle comprising a triblock copolymer, wherein said micelle has a drug-loaded inner core, a crosslinked outer core, and a hydrophilic shell, wherein the multiblock copolymer is of formula III: ##STR01635## wherein: n is 10-2500; m is 5-50; m' is 5-50; L is a metal crossliniked amino acid side-chain group; R.sup.y is a hydrophobic or ionic, natural or unnatural amino acid side-chain group; R.sup.1 is -Z(CH.sub.2CH.sub.2Y).sub.p(CH.sub.2).sub.tR.sup.3, wherein: Z is --O--; Y is --O--; p is 0-10; t is 0-10; and R.sup.3 is --N.sub.3; Q is a valence bond; R.sup.2a is --NR.sup.4C(O)R.sup.4; and each R.sup.4 is independently hydrogen or an optionally substituted aliphatic.

2. The drug-loaded micelle according to claim 1, wherein the metal is zinc.

3. The drug-loaded micelle according to claim 2, wherein the crosslinked amino acid is aspartic acid or glutamic acid.

4. The drug-loaded micelle according to claim 2, wherein the amino acid is histidine.

5. The drug-loaded micelle according to claim 1, wherein said micelle is a mixed micelle.

6. The drug-loaded micelle according to claim 1, wherein R.sup.1 is ##STR01636##

7. The drug-loaded micelle according to claim 1, wherein R.sup.2a is selected from the group consisting of: ##STR01637## ##STR01638## ##STR01639##

8. The drug-loaded micelle according to claim 1, wherein R.sup.y is a hydrophobic amino acid side-chain is a side chain of phenylalanine, alanine benzyl glutamate, alkyl glutamate, benzyl aspartate, alkyl aspartate, leucine, tyrosine, serine, threonine, glutamic acid, aspartic acid, or a combination thereof, wherein the overall amino acid side chain is hydrophobic.

9. The drug-loaded micelle according to claim 8, wherein R.sup.y is a hydrophobic amino acid side-chain selected from a mixture of phenylalanine and tyrosine or a mixture of leucine and tyrosine, such that the overall amino acid side chain is hydrophobic.

10. The drug-loaded micelle according to claim 1, wherein: n is about 200 to about 300; m is 5-25; m' is 10-50; and R.sup.2a is --NHC(O)CH.sub.3.

11. The drug-loaded micelle according to claim 1, wherein the micelle encapsulates a hydrophobic chemotherapeutic drug selected from Abarelix, Aldesleukin, Aldesleukin, Alemtuzumab, Alitretinoin, Allopurinol, Altretamine, Amifostine, Anastrozole, Arsenic trioxide, Asparaginase, Azacitidine, BCG Live, Bevacuzimab, Avastin, Fluorouracil, Bexarotene, Bleomycin, Bortezomib, Busulfan, Calusterone, Capecitabine, Camptothecin, Carboplatin, Carmustine, Celecoxib, Cetuximab, Chlorambucil, Cisplatin, Cladribine, Clofarabine, Cyclophosphamide, Cytarabine, Dactinomycin, Darbepoetin alfa, Daunorubicin, Denileukin, Dexrazoxane, Docetaxel, Doxorubicin, Doxorubicin hydrochloride, Dromostanolone Propionate, Epirubicin, Epoetin alfa, Erlotinib, Estramustine, Etoposide Phosphate, Etoposide, Exemestane, Filgrastim, floxuridine fludarabine, Fulvestrant, Gefitinib, Gemcitabine, Gemtuzumab, Goserelin Acetate, Histrelin acetate, Hydroxyurea, Ibritumomab, Idarubicin, Ifosfamide, Imatinib Mesylate, Interferon alfa-2a, Interferon alfa-2b, Irinotecan, Lenalidomide, Letrozole, Leucovorin, Leuprolide Acetate, Levamisole, Lomustine, Megestrol Acetate, Melphalan, Mercaptopurine, 6-MP, Mesna, Methotrexate, Methoxsalen, Mitomycin C, Mitotane, Mitoxantrone, Nandrolone, Nelarabine, Nofetumomab, Oprelvekin, Oxaliplatin, Paclitaxel, Palifermin, Pamidronate, Pegademase, Pegaspargase, Pegfilgrastim, Pemetrexed Disodium, Pentostatin, Pipobroman, Plicamycin, Porfimer Sodium, Procarbazine, Quinacrine, Rasburicase, Rituximab, Sargramostim, Sorafenib, Streptozocin, Sunitinib Maleate, Talc, Tamoxifen, Temozolomide, Teniposide, VM-26, Testolactone, Thioguanine, 6-TG, Thiotepa, Topotecan, Toremifene, Tositumomab, Trastuzumab, Tretinoin, ATRA, Uracil Mustard, Vairubicin, Vinbiastine, Vincristine, Vinorelbine, Zoledronate, or Zoledronic acid.

12. The drug-loaded micelle according to claim 11, wherein the hydrophobic chemotherapeutic drug is Doxorubicin or Doxorubicin hydrochloride.

13. The drug-loaded micelle according to claim 11, wherein the hydrophobic chemotherapeutic drug is Gemcitabine.

14. The drug-loaded micelle according to claim 11, wherein the hydrophobic chemotherapeutic drug is Letrozole.

Details for Patent 7,638,558

Applicant Tradename Biologic Ingredient Dosage Form BLA Approval Date Patent No. Expiredate
Recordati Rare Diseases, Inc. ELSPAR asparaginase For Injection 101063 01/10/1978 ⤷  Try a Trial 2025-04-01
Merck Teknika Llc TICE BCG bcg live For Injection 102821 06/21/1989 ⤷  Try a Trial 2025-04-01
Merck Sharp & Dohme Corp. INTRON A interferon alfa-2b For Injection 103132 06/04/1986 ⤷  Try a Trial 2025-04-01
Merck Sharp & Dohme Corp. INTRON A interferon alfa-2b For Injection 103132 ⤷  Try a Trial 2025-04-01
Merck Sharp & Dohme Corp. INTRON A interferon alfa-2b Injection 103132 ⤷  Try a Trial 2025-04-01
Amgen, Inc. EPOGEN/PROCRIT epoetin alfa Injection 103234 06/01/1989 ⤷  Try a Trial 2025-04-01
Amgen, Inc. EPOGEN/PROCRIT epoetin alfa Injection 103234 ⤷  Try a Trial 2025-04-01
>Applicant >Tradename >Biologic Ingredient >Dosage Form >BLA >Approval Date >Patent No. >Expiredate

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