- Patent Title: Remote loading of sparingly water-soluble drugs into lipid vesicles
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Application No.: US16726624Application Date: 2019-12-24
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Publication No.: US11583544B2Publication Date: 2023-02-21
- Inventor: Mark E. Hayes , Charles O. Noble , Francis C. Szoka
- Applicant: CELATOR PHARMACEUTICALS, INC.
- Applicant Address: US CA Palo Alto
- Assignee: CELATOR PHARMACEUTICALS, INC.
- Current Assignee: CELATOR PHARMACEUTICALS, INC.
- Current Assignee Address: US CA Palo Alto
- Agency: Morgan, Lewis & Bockius LLP
- Agent Jeffry S. Mann
- Main IPC: A61K9/127
- IPC: A61K9/127 ; A61K31/7048 ; A61K31/395 ; A61K31/704 ; A61K9/19 ; A61K31/337 ; A61K31/4196 ; A61K31/496 ; A61K38/07 ; A61K47/02

Abstract:
The present invention provides liposome compositions containing sparingly soluble drugs that are used to treat life-threatening diseases. A preferred method of encapsulating a drug inside a liposome is by remote or active loading. Remote loading of a drug into liposomes containing a transmembrane electrochemical gradient is initiated by co-mixing a liposome suspension with a solution of drug, whereby the neutral form of the compound freely enters the liposome and becomes electrostatically charged thereby preventing the reverse transfer out of the liposome. There is a continuous build-up of compound within the liposome interior until the electrochemical gradient is dissipated or all the drug is encapsulated in the liposome. However, this process as described in the literature has been limited to drugs that are freely soluble in aqueous solution or solubilized as a water-soluble complex. This invention describes compositions and methods for remote loading drugs with low water solubility (
Public/Granted literature
- US20210008091A1 REMOTE LOADING OF SPARINGLY WATER-SOLUBLE DRUGS INTO LIPID VESICLES Public/Granted day:2021-01-14
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