Modified drugs for use in liposomal nanoparticles
US9968554B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Jun 12, 2014 |
| Grant date | May 15, 2018 |
| Priority date | — |
| Expiry date | Jul 19, 2035 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07K7/645
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
Drag derivatives are provided herein which are suitable for loading into liposomal nanoparticle carriers. In some preferred aspects, the derivatives comprise a poorly water-soluble drag derivatized with a weak-base moiety that facilitates active loading of the drag through a LN transmembrane pH or ion gradient into the aqueous interior of the LN. The weak-base moiety can optionally comprise a lipophilic domain that facilitates active loading of the drag to the inner monolayer of the liposomal membrane. Advantageously, LN formulations of the drag derivatives exhibit improved solubility, reduced toxicity, enhanced efficacy, and/or other benefits relative to the corresponding free drags.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.