US 12,433,874 B2
Liposome comprising rapamycin or a derivative thereof and use thereof in therapy
Tzu-Ying Tseng, Taipei (TW)
Assigned to PRESCIENCE BIOTECHNOLOGY INC., Taipei (TW)
Filed by PRESCIENCE BIOTECHNOLOGY INC., Taipei (TW)
Filed on Apr. 28, 2022, as Appl. No. 17/661,153.
Prior Publication US 2023/0346754 A1, Nov. 2, 2023
Int. Cl. A61K 31/436 (2006.01); A61K 9/1271 (2025.01); A61K 47/24 (2006.01); A61K 47/26 (2006.01); A61K 47/28 (2006.01); A61P 35/00 (2006.01)
CPC A61K 31/436 (2013.01) [A61K 9/1271 (2013.01); A61K 47/24 (2013.01); A61K 47/26 (2013.01); A61K 47/28 (2013.01); A61P 35/00 (2018.01)] 9 Claims
 
1. A liposome comprising a lipid ingredient encapsulating rapamycin or an analog thereof, or a prodrug or salt of rapamycin or its analog,
wherein: the lipid ingredient is:
(1) a combination of dipalmitoylphosphatidylcholine (DPPC), 1,2-Didecanoyl-sn-glycero-3-phosphocholine (DDPC), and PEGlated 1,2-Distearoyl-sn-glycero-3-phosphorylethanolamine (DSPE-PEG),
wherein (a) the DPPC, DDPC, and DSPE-PEG are respectively present in an amount of about 35% (w/w), about 27% (w/w), and about 23% (w/w), based on the dry weight of the total amount of the liposome, or (b) the DPPC, DDPC, and DSPE-PEG are present in a weight ratio of about 2.4:1.9:1.6; or
(2) a combination of DOPE (dioleoyl phosphatidyl ethanolamine), DDPC, and DSPE-PEG,
wherein (a) the DOPE, DDPC, and DSPE-PEG are respectively present in an amount of about 35% (w/w), about 27% (w/w), and about 23% (w/w), based on the dry weight of the total amount of the liposome, or (b) the DOPE, DDPC, and DSPE-PEG are present in a weight ratio of about 2.4:1.8:1.6;
the rapamycin analog is able to inhibit a mammalian target of rapamycin (mTOR); and
the amount of rapamycin or an analog thereof, or a prodrug or salt of rapamycin or its analog, based on the dry weight of the total amount of liposome, ranges from about 10% (w/w) to 25% (w/w).