LIPID GROWTH FACTOR FORMULATIONS
First Claim
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1. An aqueous colloidal lipid microparticle (LMP) pharmaceutical composition comprising a therapeutic compound, a lipid carrier, and an emulsifying agent.
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Abstract
The present invention is directed to novel formulations and methods for the improved delivery and administration of hydrophobic therapeutic compounds that are substantially insoluble and/or susceptible to precipitation in aqueous solution at physiological pH, including, e.g., growth and differentiation factor-5 and related proteins. Many therapeutic compounds are hydrophobic at physiological pH levels.
75 Citations
62 Claims
- 1. An aqueous colloidal lipid microparticle (LMP) pharmaceutical composition comprising a therapeutic compound, a lipid carrier, and an emulsifying agent.
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23. A method for the prevention of precipitation of a therapeutic agent in blood and/or aqueous solutions at a pH between 4.0 and 8.5.
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24. A method for increasing solubility of a therapeutic agent that is hydrophobic and substantially insoluble and/or susceptible to precipitation in aqueous media at physiological pH, comprising
a) dissolving the therapeutic agent in aqueous buffer at a non-physiological pH; -
b) lyophilizing the therapeutic agent solution; c) preparing a colloidal therapeutic agent carrier solution comprising a lipid carrier and an emulsifying agent; d) ensuring the colloidal therapeutic agent carrier solution has a pH that is substantially the same as the pH of the therapeutic agent dissolved in aqueous buffer; e) combining the lyophilized therapeutic agent solution and the colloidal therapeutic agent carrier solution; and f) adjusting the pH of the combined lyophilized therapeutic agent solution and the colloidal therapeutic agent carrier solution to physiological pH to create a pharmaceutical composition. - View Dependent Claims (28)
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49. A method for targeting delivery of a therapeutic agent to the rear of the brain, comprising
a) dissolving the therapeutic agent in aqueous buffer; -
b) lyophilizing the therapeutic agent solution; c) preparing a colloidal therapeutic agent carrier solution comprising a lipid carrier and an emulsifying agent; d) ensuring the colloidal therapeutic agent carrier solution has a pH that is substantially the same as the pH of the therapeutic agent dissolved in aqueous buffer; e) combining the lyophilized therapeutic agent solution and the colloidal therapeutic agent carrier solution to create a pharmaceutical composition; and f) increasing the viscosity of the pharmaceutical composition to reduce delivery of the pharmaceutical composition to the olfactory epithelium and the olfactory bulbs and rostral brain structures and to target delivery of the pharmaceutical composition to the respiratory epithelium, trigeminal nerve, caudal brain structures, upper spinal cord, meninges and lymphatics.
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Specification