Dry powder formulation of caveolin-1 peptides and methods of use thereof
Inventors
Williams, III, Robert O. • Watts, Alan B. • Zhang, Yajie • SAHAKIJPIJARN, Sawittree • Christensen, Dale • Koleng, John J.
Assignees
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Publication Number
US-12280088-B2
Publication Date
2025-04-22
Expiration Date
Abstract
Provided herein are compositions comprising caveolin-1 (Cav-1) peptides. Further provided are methods of using the Cav-1 peptides for the treatment of lung infections or acute or chronic lung injury, particularly lung fibrosis.
Core Innovation
The invention relates to Cav-1 (caveolin-1) peptide therapeutics formulated as a dry powder composition for use in a dry powder inhaler. The particles comprise a peptide consisting of FTTFTVT (SEQ ID NO: 2) or a pharmaceutically acceptable salt thereof, and the dry powder composition does not comprise a pharmaceutically acceptable carrier or excipient. The composition is characterized by a median particle diameter of less than 5 cm.
The disclosure includes formulations based on Cav-1 scaffolding domain peptide sequences and pharmaceutically acceptable salts, including peptide variants (SEQ ID NOs 2-20) and optional cell penetrating peptides (CPPs). The peptide therapeutics are described in an essentially excipient-free format with low water content, and the formulations include approaches for preparing dry powders, including milling processes and powder-forming routes.
The invention also includes characterization and performance testing of the dry powders for inhalation, including particle properties and aerosol performance metrics. Longer-term stability is described for milled Cav-1 peptide ammonium counterion formulations, including encapsulated versus bulk powder embodiments, and in vivo results are reported using a bleomycin lung fibrosis model following dry powder inhalation.
Claims Coverage
The document contains one independent claim (clm-00001). It claims a dry powder composition defined by peptide identity, particle size, absence of pharmaceutically acceptable carrier/excipient, and formulation for a dry powder inhaler; dependent claims refine salt form, particle size metrics/distributions, production/stability scope, and inhalation/device-related scope.
Cav-1 peptide particles in a dry powder inhaler formulation
Particles comprise a peptide consisting of FTTFTVT (SEQ ID NO: 2) or a pharmaceutically acceptable salt thereof, and the dry powder composition is formulated for use in a dry powder inhaler.
Small median particle diameter without pharmaceutically acceptable carrier or excipient
The particles have a median particle diameter of less than 5 cm, and the dry powder composition does not comprise a pharmaceutically acceptable carrier or excipient.
Ammonium salt dry powder refinement
The dry powder composition further specifies that the particles comprise a pharmaceutically acceptable ammonium salt as the salt form.
Controlled particle size distribution
At least 70% of the particles have a particle size of about 1 cm to about 5 cm.
Median particle diameter defined as MMAD
The composition specifies that the dry powder particles median diameter is specified as a mass median aerodynamic diameter (MMAD).
Air jet milling production refinement
A dry powder composition is produced by air jet milling.
At least 6-month stability
The dry powder composition remains stable for at least 6 months.
Overall, the claim set is directed to an essentially carrier/excipient-free dry powder inhaler composition containing Cav-1 peptide FTTFTVT (SEQ ID NO: 2) or pharmaceutically acceptable salts, with a sub-5 cm median particle diameter, and with dependent claim refinements including ammonium salt selection, specified particle size metrics/distributions, air jet milling, and stability for at least 6 months.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Not explicitly described in patent.
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