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    Modulation of drug loading in multivescular liposomes
    52.
    发明授权
    Modulation of drug loading in multivescular liposomes 失效
    多重脂质体中药物负载的调节

    公开(公告)号：US6106858A

    公开(公告)日：2000-08-22

    申请号：US925532

    申请日：1997-09-08

    申请人： Qiang Ye ,  Nandini Katre ,  Mantripragada Sankaram

    发明人： Qiang Ye ,  Nandini Katre ,  Mantripragada Sankaram

    IPC分类号： A61K9/127 ,  A61K31/485 ,  A61K31/7068 ,  A61K38/04 ,  A61K38/22 ,  A61K38/24 ,  A61K45/00 ,  A61K47/04 ,  A61K47/06 ,  A61K47/10 ,  A61K47/12 ,  A61K47/14 ,  A61K47/16 ,  A61K47/18 ,  A61K47/26 ,  A61K47/36 ,  A61P3/10 ,  A61P5/00 ,  A61P9/00 ,  A61P9/04 ,  A61P9/06 ,  A61P9/12 ,  A61P11/06 ,  A61P23/00 ,  A61P25/04 ,  A61P25/20 ,  A61P25/22 ,  A61P29/00 ,  A61P31/10 ,  A61P31/12 ,  A61P35/00 ,  A61P37/02

    CPC分类号： A61K9/127

    摘要： Disclosed is a method for making liposomes, for example multivesicular liposomes (MVLs), containing one or more biologically active agents, wherein the loading of the active agents into the liposomes is modulated by adjusting the osmolarity of the aqueous component into which the agents are dissolved prior to encapsulation. To increase the loading of the active agent, the osmolarity of the aqueous component is reduced, and to decrease the loading of the active agent, the osmolarity of the aqueous component is increased. In the making of MVLs, the process involves dissolving the active agent and an optional osmotic excipient in a first aqueous component encapsulated within the liposomes. For any given concentration of drug, the osmolarity of the first aqueous component can be adjusted by increasing or decreasing the concentration or molecular weight of the osmotic excipients used therein. The rate of release of the active agent into the surrounding environment in which the liposomes are introduced can be simultaneously controlled by incorporating into the lipid component used in the formulation at least one long chain amphipathic lipid. For example, the amphipathic lipid can have from about 13 to about 28 carbons in its carbon chain. Use of the long chain amphipathic lipid in the lipid component is particularly helpful in controlling the release rate and encapsulation efficiency for high drug load formulations.

    摘要翻译： 公开了一种制备脂质体的方法，例如含有一种或多种生物活性剂的多泡脂质体（MVL），其中通过调节试剂溶解于其中的水性组分的渗透压来调节活性剂向脂质体中的负载 在封装之前。 为了增加活性剂的负载量，水性组分的渗透压降低，并且为了降低活性剂的负载量，水性组分的渗透压增加。 在制备MVL时，该方法包括将活性剂和任选的渗透性赋形剂溶解在包封在脂质体内的第一含水组分中。 对于任何给定的药物浓度，可以通过增加或降低其中使用的渗透性赋形剂的浓度或分子量来调节第一含水组分的渗透压。 引入脂质体的周围环境中活性剂的释放速率可以通过将至少一种长链两亲性脂质掺入用于制剂中的脂质组分中来同时控制。 例如，两亲性脂质在其碳链中可以具有约13至约28个碳。 在脂质组分中使用长链两亲脂质特别有助于控制高药物负荷制剂的释放速率和包封效率。