Esterification/saponification-based method for liposomal encapsulation of hydrophilic glucuronides
US11013690B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Jan 4, 2017 |
| Grant date | May 25, 2021 |
| Priority date | — |
| Expiry date | Jan 4, 2037 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61P35/00
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
Described herein is a method for loading a hydrophilic compound into liposomes after addition of an alkylester group to form an esterified compound. After loading, the alkylester is hydrolyzed to reform the hydrophilic compound inside the liposomes. Also described is a method for loading drugs under a glucuronide methylester form into liposomes. The glucuronide methylester form of the drug is saponified to a glucuronide form of the drug inside the liposomes for better drug retention. The glucuronide residue conjugated to drugs can be removed inside cells to regenerate the parental drug upon cell uptake, liposomal degradation and enzyme hydrolysis. In case of cancer, this method can be used to safely deliver drugs to tumors.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.