Intracutaneous paste composition
View Patent ↗The delivery of biopharmaceutical and other therapeutic agents parenterally to an animal via a minimally invasive, low pain administration is provided. The agents are delivered to the patient via, e.g., the epidermal, dermal, or subcutaneous layer of the skin in a concentrated fours of injectable paste of slurry.
1. A composition for intracutaneous injection of a therapeutic agent, said composition comprising an effective amount of said therapeutic agent in the form of a powder, wherein said powder is homogeneously contained within a pharmaceutically acceptable carrier, wherein said composition comprises 0.1 to about 1000 microliters, and wherein said composition is concentrated in the form of a stable paste suitable for intracutaneous injection.
2. The composition of claim 1 , wherein said paste is a slurry.
3. The composition of claim 1 , wherein said therapeutic agent is a protein, peptide or polypeptide.
4. The composition of claim 3 , wherein said therapeutic agent is a peptide.
5. The composition of claim 4 , wherein said peptide is glucagon.
6. The composition of claim 1 , wherein said powder is prepared by subjecting the therapeutic agent to lyophilization, spray-drying, freeze-drying, spray-freeze drying or a combination thereof prior to incorporation into said pharmaceutically acceptable carrier.
7. The composition of claim 6 , wherein said powder has a mean particle size ranging from 10 nanometers (0.01 microns) to about 100 microns, with no particles being larger than about 500 microns.
8. The composition of claim 1 , further comprising an effective amount of a stabilizing agent.
9. The composition of claim 8 , wherein said stabilizing agent is a member selected from the group consisting of surfactants, polyoxamers, polyols, gels, amphoteric compounds, and mixtures thereof.
10. The composition of claim 1 , wherein said therapeutic agent is stable in said formulation for at least about 2 months when said composition is stored at room temperature.
11. The composition of claim 1 , wherein said pharmaceutically acceptable carrier is a non-aqueous or semi-aqueous carrier.
12. The composition of claim 11 , wherein said pharmaceutically acceptable carrier is a non-aqueous carrier.
13. The composition of claim 12 , wherein said pharmaceutically acceptable carrier is selected from the group consisting of alkyl benzoates, aryl benzoates, aralkyl benzoates, triacetin, dimethyl sulfoxide (DMSO), N-methyl -2- pyrrolidone (NMP), and mixtures thereof.
14. The composition of claim 1 , wherein said composition comprises about 1 microliter to about 250 microliters.
15. The composition of claim 1 , wherein said composition further comprises a pharmaceutically acceptable polymer that imparts thixotropic properties to said composition.
16. The composition of claim 1 , wherein said composition further comprises a pharmaceutically acceptable polymer in an amount effective to slow the release of said therapeutic agent from said composition upon intracutaneous injection.
17. The composition of claim 1 , wherein said therapeutic agent is incorporated into liposomes or conjugated to or incorporated with polysaccharides and/or other polymers to provide a controlled release of said therapeutic agent from said formulation upon intracutaneous injection.