发明名称 |
LIPOSOMES CO-ENCAPSULATING A BISPHOSPHONATE AND AN AMPHIPATHIC AGENT |
摘要 |
The present disclosure provides liposomes comprising a membrane and an intraliposomal aqueous water phase, the membrane comprising at least one liposome forming lipid and the intraliposomal aqueous water phase comprises a salt of a bisphosphonate together with an amphipathic weak base agent (PLAD). An example of a liposome is one comprising co encapsulated in the intraliposomal aqueous water phase N-containing bisphosphonate, such as alendronate, and an anthracycline such as doxorubicin which was shown to increase survival as compared to Doxil or to administrations of liposomal alendronate (PLA) and Doxil (separate liposomes). Such liposomes may carry a targeting moiety exposed at the liposome's outer surface, for example, conjugate of folic acid as a targeting moiety to folate receptor (FT-PLAD). Also provided by the present disclosure is a method of preparing the liposomes and methods of use of the liposomes, at times, in combination with additional active ingredients, such as γδ T-cells. |
申请公布号 |
US2014328899(A1) |
申请公布日期 |
2014.11.06 |
申请号 |
US201214232332 |
申请日期 |
2012.07.07 |
申请人 |
Gabizon Alberto A.;Barenholz Yechezkel;Shmeeda Hilary |
发明人 |
Gabizon Alberto A.;Barenholz Yechezkel;Shmeeda Hilary |
分类号 |
A61K9/127;A61K31/663;A61K31/704;A61K35/14 |
主分类号 |
A61K9/127 |
代理机构 |
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代理人 |
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主权项 |
1. A liposome comprising a membrane and an intraliposomal aqueous water phase, the membrane comprising at least one liposome forming lipid and the intraliposomal aqueous water phase comprising a salt of a bisphosphonate and an amphipathic weak base agent having a pKa equal or below 11 and a log D at pH 7 in the range between −2.5 and 1.5. |
地址 |
Jerusalem IL |