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    Blood-stable, cholesterol-free liposomes
    3.
    发明授权
    Blood-stable, cholesterol-free liposomes 失效
    血液稳定，无胆固醇的脂质体

    公开(公告)号：US5043164A

    公开(公告)日：1991-08-27

    申请号：US298452

    申请日：1989-01-17

    申请人： Leaf Huang ,  Dexi Liu

    发明人： Leaf Huang ,  Dexi Liu

    IPC分类号： A61K9/127 ,  A61K9/133

    CPC分类号： A61K9/1275 ,  A61K9/127 ,  Y10S436/829 ,  Y10S514/97 ,  Y10S514/971 ,  Y10T428/2984

    摘要： Small unilamellar liposomes (d

    摘要翻译： 通过向新制备的脂质体悬浮液中加入包含不饱和磷脂酰乙醇胺（PE）如二油酰PE（DOPE）和脂肪酸如油酸（OA）的小单层脂质体（d <600nm）），其具有 形成胶束的高趋势。 示出了以下胶束形成两亲物的实例：溶血磷脂，神经节苷脂（GM1和GT1b），硫苷脂，合成糖脂如唾液酸乳糖基磷脂酰乙醇胺，亲水药物如胞嘧啶阿拉伯糖二磷酸二甘油，和蛋白质如细胞色素b5，人高密度 脂蛋白（HDL）和人血型糖蛋白A。稳定的脂质体对白蛋白的溶解作用有抗性，白蛋白是导致这种脂质体裂解的主要血液成分。 在本发明之前，包含PE和OA的脂质体通常通过掺入胆固醇来稳定。

    Liposomal vectors
    4.
    发明申请
    Liposomal vectors 审中-公开
    脂质体载体

    公开(公告)号：US20060062841A1

    公开(公告)日：2006-03-23

    申请号：US11219507

    申请日：2005-09-01

    申请人： Leaf Huang ,  Feng Liu

    发明人： Leaf Huang ,  Feng Liu

    IPC分类号： A61K48/00 ,  A61K9/127 ,  C12N15/88 ,  A61K36/37

    CPC分类号： C12N15/88 ,  A61K9/1272 ,  A61K31/573 ,  A61K36/24 ,  A61K36/37 ,  A61K45/06 ,  A61K48/00 ,  A61K48/0033 ,  A61K2300/00

    摘要： The present invention provides for liposomal vectors which inhibit inflammation and/or enhance expression of transferred genes. It is based, at least in part, of the discovery that vectors comprising a nucleic acid carrying a gene of interest and a cationic liposome containing an immunosuppressive agent induce lower levels of inflammatory cytokine relative to conventional lipolex vectors, as well as on the discovery that a component may be incorporated into the liposome which enhances expression of the gene of interest.

    摘要翻译： 本发明提供抑制炎症和/或增强转移基因表达的脂质体载体。 至少部分地基于以下发现：包含携带目的基因的核酸的载体和含有免疫抑制剂的阳离子脂质体相对于常规的lipolex载体诱导较低水平的炎症细胞因子，以及发现 可以将一种成分掺入脂质体中，从而增强感兴趣的基因的表达。

    Sphingomyelin liposomes for the treatment of hyperactive bladder disorders
    5.
    发明授权
    Sphingomyelin liposomes for the treatment of hyperactive bladder disorders 有权
    鞘磷脂脂质体用于治疗膀胱过动症

    公开(公告)号：US08110217B2

    公开(公告)日：2012-02-07

    申请号：US11546025

    申请日：2006-10-11

    申请人： Michael B. Chancellor ,  Pradeep Tyagi ,  Matthew O. Fraser ,  Yao-Chi Chuang ,  William C de Groat ,  Leaf Huang ,  Naoki Yoshimura

    发明人： Michael B. Chancellor ,  Pradeep Tyagi ,  Matthew O. Fraser ,  Yao-Chi Chuang ,  William C de Groat ,  Leaf Huang ,  Naoki Yoshimura

    IPC分类号： A61K9/127

    CPC分类号： A61K9/127 ,  A61K9/0034 ,  A61K9/1272 ,  Y02A50/469

    摘要： The present invention provides pharmaceutical compositions and methods for the instillation of lipid vehicles comprised of liposomes containing sphingomyelin or sphingomyelin metabolites to prevent, manage, ameliorate and/or treat disorders involving neuropathic pain and aberrant muscle contractions, such as what occurs in bladder hyperactivity disorders such as interstitial cystitis (IC) in animals or humans in need thereof. Also provided is a liposome-based delivery of drugs, e.g., antibiotics, pain treatments and anticancer agents, to the bladder, genitourinary tract, gastrointestinal system, pulmonary system and other organs or body systems. In particular, liposome-based delivery of vanilloid compounds, such as resiniferatoxin, capsaicin, or tinyatoxin and toxins, such as botulinum toxin is provided for the treatment of bladder conditions, including pain, inflammation, incontinence and voiding dysfunction.

    摘要翻译： 本发明提供用于滴注含有鞘磷脂或鞘磷脂代谢物的脂质体的脂质载体的药物组合物和方法，以预防，治疗，改善和/或治疗涉及神经性疼痛和异常肌肉收缩的疾病，例如膀胱多动障碍 作为有需要的动物或人类的间质性膀胱炎（IC）。 还提供了对膀胱，泌尿生殖道，胃肠系统，肺系统和其他器官或身体系统的基于脂质体的药物递送，例如抗生素，疼痛治疗和抗癌剂。 特别地，提供了基于脂质体的递送香草素化合物，例如树脂毒素，辣椒素或微量毒素和毒素，例如肉毒杆菌毒素，用于治疗膀胱状况，包括疼痛，炎症，失禁和排尿功能障碍。

    Stable aqueous dispersions including cationic lipids
    7.
    发明授权
    Stable aqueous dispersions including cationic lipids 失效
    稳定的水分散体包括阳离子脂质

    公开(公告)号：US06361791B1

    公开(公告)日：2002-03-26

    申请号：US08580779

    申请日：1995-12-28

    申请人： Leaf Huang ,  Richard M. Epand ,  Remo Bottega

    发明人： Leaf Huang ,  Richard M. Epand ,  Remo Bottega

    IPC分类号： A61K9127

    CPC分类号： C07J41/0055 ,  A61K9/1272 ,  A61K47/54 ,  A61K47/554 ,  C07J9/00 ,  C12N15/64 ,  C12N15/88 ,  Y10T428/2984

    摘要： A stable aqueous dispersion which comprises a cationic lipid which is a molecule which comprises a cholesterol-derived lipophilic group, a linker bond which is hydrolyzable by cellular enzymes and relatively resistant to base-catalyzed hydrolysis, a spacer arm and a cationic amino group, and an appropriate co-lipid. The invention also includes the cationic lipids and mammalian plasmid DNA or other cells in admixture with the aqueous dispersion.

    摘要翻译： 一种稳定的水分散体，其包含阳离子脂质，其是包含胆固醇衍生的亲脂基团的分子，可被细胞酶水解并且相对抗碱基催化水解的连接体键，间隔臂和阳离子氨基，以及 合适的辅助脂质。 本发明还包括与水分散体混合的阳离子脂质和哺乳动物质粒DNA或其它细胞。

    Fused liposome and acid induced method for liposome fusion
    8.
    发明授权
    Fused liposome and acid induced method for liposome fusion 失效
    融合脂质体和酸诱导的脂质体融合方法

    公开(公告)号：US5283122A

    公开(公告)日：1994-02-01

    申请号：US836125

    申请日：1992-02-14

    申请人： Leaf Huang ,  Jerome Connor

    发明人： Leaf Huang ,  Jerome Connor

    IPC分类号： A61K9/127 ,  C12N15/88

    CPC分类号： A61K9/1272 ,  C12N15/88 ,  Y10S436/829 ,  Y10T428/2984

    摘要： Liposomes containing phosphatidylethanolamine, palmitoyl homocysteine or oleic acid or palmitic acid, fuse rapidly when the pH of the medium is reduced below 7. Liposome fusion was measured by (a) mixing of the liposomal lipids as shown by resonance energy transfer, (b) gel filtration and (c) electron microscopy. The presence of phosphatidylethanolamine or acid addition esters thereof in the liposomes greatly enhances fusion; whereas the presence of phosphatidylcholine inhibits fusion. During fusion of liposomes containing phosphatidylethanolamine:palmitoyl homocysteine (8:2), almost all of the encapsulated calcein is released. Inclusion of cholesterol (40%) in the liposomes substantially decreases leakage without impairing fusion. Those pH sensitive liposomes are fused to deliver biologically active molecules such as DNA, into living cells.

    摘要翻译： 含有磷脂酰乙醇胺，棕榈酰高半胱氨酸或油酸或棕榈酸的脂质体当培养基的pH值降至7以下时迅速融合。脂质体融合通过（a）如共振能量转移所示脂质体脂质的混合，（b）凝胶 过滤和（c）电子显微镜。 磷脂酰乙醇胺或其酸加成酯在脂质体中的存在大大增强了融合; 而磷脂酰胆碱的存在抑制融合。 在含有磷脂酰乙醇胺的脂质体融合过程中，棕榈酰同型半胱氨酸（8：2）几乎全部被包裹的钙黄绿素释放出来。 在脂质体中包含胆固醇（40％）可显着减少渗漏而不损害融合。 将这些pH敏感的脂质体融合以将生物活性分子例如DNA递送到活细胞中。

    Fused liposome and acid induced method for liposome fusion
    9.
    发明授权
    Fused liposome and acid induced method for liposome fusion 失效
    融合脂质体和酸诱导的脂质体融合方法

    公开(公告)号：US4789633A

    公开(公告)日：1988-12-06

    申请号：US602177

    申请日：1984-04-19

    申请人： Leaf Huang ,  Jerome Connor

    发明人： Leaf Huang ,  Jerome Connor

    IPC分类号： A01H1/00 ,  A01H5/00 ,  A61K9/00 ,  A61K9/127 ,  B01J13/02 ,  C12N5/00 ,  C12N5/02 ,  C12N5/10 ,  C12N15/00 ,  C12N15/88 ,  A61J5/00 ,  B32B5/16

    CPC分类号： A61K9/127 ,  A61K9/1272 ,  C12N15/88 ,  Y10T428/2984

    摘要： Liposomes containing phosphatidylethanolamine, palmitoyl homocysteine or oleic acid or palmitic acid, fuse rapidly when the pH of the medium is reduced below 7. Liposome fusion was measured by (a) mixing of the liposomal lipids as shown by resonance energy transfer, (b) gel filtration and (c) electron microscopy. The presence of phosphatidylethanolamine or acid addition esters thereof in the liposomes greatly enhances fusion; whereas the presence of phosphatidylcholine inhibits fusion. During fusion of liposomes containing phosphatidylethanolamine:palmitoyl homocysteine (8:2), almost all of the encapsulate calcein is released. Inclusion of cholesterol (40%) in the liposomes substantially decreases leakage without impairing fusion. Those pH sensitive liposomes are fused to deliver biologically active molecules such as DNA, into living cells.

    摘要翻译： 含有磷脂酰乙醇胺，棕榈酰高半胱氨酸或油酸或棕榈酸的脂质体当培养基的pH值降至7以下时迅速融合。脂质体融合通过（a）如共振能量转移所示脂质体脂质的混合，（b）凝胶 过滤和（c）电子显微镜。 磷脂酰乙醇胺或其酸加成酯在脂质体中的存在大大增强了融合; 而磷脂酰胆碱的存在抑制融合。 在含有磷脂酰乙醇胺的脂质体融合过程中，棕榈酰同型半胱氨酸（8：2）几乎全部释放出钙黄绿素。 在脂质体中包含胆固醇（40％）可显着减少渗漏而不损害融合。 将这些pH敏感的脂质体融合以将生物活性分子例如DNA递送到活细胞中。

    Liposomes comprising a calcium phosphate-containing precipitate
    10.
    发明授权
    Liposomes comprising a calcium phosphate-containing precipitate 有权

    公开(公告)号：US09937128B2

    公开(公告)日：2018-04-10

    申请号：US13388538

    申请日：2010-08-03

    申请人： Leaf Huang ,  Jun Li

    发明人： Leaf Huang ,  Jun Li

    IPC分类号： A61K9/127 ,  A61K48/00 ,  C12N15/11

    CPC分类号： A61K9/1271 ,  A61K9/1277 ,  A61K48/0025 ,  C12N15/111 ,  C12N2310/14 ,  C12N2310/3515 ,  C12N2320/32

    摘要： Provided herein are methods and compositions for the delivery of bioactive compounds to a cell, tissue, or physiological site. The compositions comprise delivery system complexes comprising liposomes encapsulating a biodegradable ionic precipitate having incorporated therein a bioactive compound and delivery system complexes comprising a biodegradable ionic precipitate ionically bound to a surrounding lipid bilayer, wherein the biodegradable ionic precipitate comprises a bioactive compound. Also provided herein are methods for the treatment of a disease or an unwanted condition in a subject, wherein the methods comprise administering the delivery system complexes comprising bioactive compounds that have therapeutic activity against the disease or unwanted condition to the subject.