Remote loading of sparingly water-soluble drugs into liposomes
US9737485B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Jul 21, 2016 |
| Grant date | Aug 22, 2017 |
| Priority date | — |
| Expiry date | Jul 21, 2036 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61K9/19
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
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 (<2 mg/mL). In the preferred embodiment the drug in the solubilizing agent is mixed with the liposomes in aqueous suspension so that the concentration of solubilizing agent is lowered to below its cap…
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.