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公开(公告)号：US20220071917A9
公开(公告)日：2022-03-10
申请号：US16760527
申请日：2018-11-02
发明人： María José Alonso Fernandez , Desireé Teijeiro Osorio , Carmen María Teijeiro Valiño , Ana Cadete Pires
IPC分类号： A61K9/51 , C07K16/22 , A61K39/395 , A61K47/62 , A61K47/69
摘要： The present invention generally relates to particles, including nanocapsules or other nanoentities, comprising a polymer such as polysialic acid. The particles are able to access the interior of the cells, and/or to procure the intracellular release of the associated drugs. In 5 one aspect, the present invention is directed to nanocapsules or other entities having an exterior or surface comprising a polymer such as polysialic acid. In some cases, targeting moieties such as Lyp-1 or tLyp-1 peptide are bonded to the polymer, e.g., using aminoalkyl (C1-C4) succinimide or other linkers. These may be created, for example, by reacting a carboxylate moiety on a polymer with an aminoalkyl maleimide (C1-C4) or an aminoalkyl 10 (C1-C4) methacrylamide, and reacting the resulting aminoalkyl (C1-C4) maleimide or the aminoalkyl (C1-C4) methacrylamide to a cysteine or other sulfur group. Targeting moieties are bonded to the polymer, for example, by reacting a carboxylate moiety on a polymer with a N-hydroxysuccinimide or a carbodiimide, and reacting the intermediate formed with a lysine or arginine group on a targeting peptide to produce polymer-amide-peptide. Other 15 aspects of the invention are generally directed to methods of making or using such compositions, kits including such compositions, or the like.
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公开(公告)号：US20210228494A1
公开(公告)日：2021-07-29
申请号：US16760527
申请日：2018-11-02
发明人： María José Alonso Fernandez , Desireé Teijeiro Osorio , Carmen María Teijeiro Valiño , Ana Cadete Pires
IPC分类号： A61K9/51 , C07K16/22 , A61K39/395 , A61K47/62 , A61K47/69
摘要： The present invention generally relates to particles, including nanocapsules or other nanoentities, comprising a polymer such as polysialic acid. The particles are able to access the interior of the cells, and/or to procure the intracellular release of the associated drugs. In 5 one aspect, the present invention is directed to nanocapsules or other entities having an exterior or surface comprising a polymer such as polysialic acid. In some cases, targeting moieties such as Lyp-1 or tLyp-1 peptide are bonded to the polymer, e.g., using aminoalkyl (C1-C4) succinimide or other linkers. These may be created, for example, by reacting a carboxylate moiety on a polymer with an aminoalkyl maleimide (C1-C4) or an aminoalkyl 10 (C1-C4) methacrylamide, and reacting the resulting aminoalkyl (C1-C4) maleimide or the aminoalkyl (C1-C4) methacrylamide to a cysteine or other sulfur group. Targeting moieties are bonded to the polymer, for example, by reacting a carboxylate moiety on a polymer with a N-hydroxysuccinimide or a carbodiimide, and reacting the intermediate formed with a lysine or arginine group on a targeting peptide to produce polymer-amide-peptide. Other 15 aspects of the invention are generally directed to methods of making or using such compositions, kits including such compositions, or the like.
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公开(公告)号：US20220177603A1
公开(公告)日：2022-06-09
申请号：US17602061
申请日：2020-04-30
摘要： Provided herein is a composition, comprising: a plurality of nanoentities comprising an inner core surrounded by an outer shell, the outer shell comprising a polymer, the inner core comprising at least one hydrophobic compound, wherein the nanoentities comprise a pharmaceutical agent, wherein the pharmaceutical agent is an antibody or a fragment thereof, wherein the antibody or the fragment thereof binds to an epitope of an activated mutated KRAS protein. These anti-KRAS antibodies formulated into particular nanoentities are able to be intracellular delivered and further, are able to perform their biological activity inside the cell, thus being useful in the treatment of cancer and other disease associated with a mutation in a KRAS gene.
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