US 11,534,399 B2 · Inhalable liposomal sustained release composition for use in treating pulmonary diseases

Abstract

Provided is a liposomal sustained-release composition for use in treatment of pulmonary disease. The liposomal sustained release composition comprises a liposome that includes a polyethylene glycol (PEG)-modified lipid and encapsulates a tyrosine kinase inhibitor. Tyrosine kinase inhibitor is stably entrapped in the liposome, and the resulting liposomal drug formulation can be aerosolized or nebulized for administration via inhalation. This aerosolized liposomal drug formulation yields consistent pharmacokinetic and pharmacodynamic profiles while achieving desired efficacy and safety.

Claims17

Dependent claims

A liposomal sustained-release composition for use in the treatment of a pulmonary disease via inhalation, comprising liposomes having entrapped nintedanib, wherein each liposome comprises:

a lipid bilayer comprising one or more phospholipids, a sterol, and a polyethylene glycol (PEG)-modified lipid;
and
an aqueous interior encompassed by the lipid bilayer and entrapping the nintedanib;
wherein the liposomes have a mean particle diameter between about 50 nm and about 400 nm;
and
wherein the composition has a ratio of nintedanib-to-phospholipid from about 0.1 mol nintedanib/mol phospholipid to about 2.5 mol nintedanib/mol phospholipid.

3 more elements

Dependencies are inferred from the claim text.

Facts

Application

17/045,940Filed 23 Apr 2019 · us provisional application

Priority

23 Apr 2018

Published

US 2021/0145740 A120 May 2021

Granted

27 Dec 2022

Term ends

Not estimatedThe source records don’t support an estimate.

Classification7 codes

A61K 9/0078
Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy: for inhalation via a nebulizer…
A61K 9/1272
Non-conventional liposomes, e.g. PEGylated liposomes or liposomes coated or grafted with polymers: comprising non-phosphatidyl surfactants as…
A61K 31/496
Having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines: non-condensed piperazines…
A61K 47/20
Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite: containing sulfur, e.g. dimethyl…

Inhalable liposomal sustained release composition for use in treating pulmonary diseases

Life of this patent

Inhalable liposomal sustained release composition for use in treating pulmonary diseases

Life of this patent

Abstract

Claims17