Methods of assessing suitability of use of pharmaceutical compositions of albumin and poorly water soluble drug
Inventors
Peykov, Viktor • Foss, Willard • Pierce, Daniel W. • Desai, Neil P.
Assignees
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Publication Number
US-10705070-B1
Publication Date
2020-07-07
Expiration Date
Abstract
The present invention provides methods of assessing suitability of a pharmaceutical composition for medical use. The pharmaceutical composition comprises nanoparticles comprising rapamycin coated with albumin and a non-nanoparticle portion comprising albumin and rapamycin.
Core Innovation
The invention relates to assessing suitability of a pharmaceutical composition for medical use in a human individual, where the pharmaceutical composition comprises nanoparticles comprising rapamycin coated with a coating comprising albumin and a non-nanoparticle portion comprising albumin and rapamycin. The method separates the nanoparticles from the non-nanoparticle portion and measures albumin species within the albumin coating of the separated nanoparticles to determine whether the composition is suitable for medical use.
In particular, one approach measures a weight percentage of albumin in the form of albumin polymers among the total albumin in the coating of the separated nanoparticles, and suitability is indicated when the weight percentage of albumin polymers is from about 15% to about 40%. Another approach measures a weight percentage of albumin in the form of albumin monomers among the total albumin in the coating of the separated nanoparticles, and suitability is indicated when the weight percentage of albumin monomers is from about 40% to about 60%.
The document further describes albumin oligomeric status and related physicochemical and functional attributes, including albumin species distributions, nanoparticle morphology and albumin coating thickness, rapamycin solubility and crystallinity, rapamycin recovery after filtration, and albumin-rapamycin binding affinity. It also describes validating commercial batches by sampling and assessing suitability, including measurement of albumin monomer, polymer, and oligomer fractions and related characterization attributes.
Claims Coverage
The patent includes at least two independent claims. The inventive features focus on separating rapamycin-coated albumin nanoparticles from a non-nanoparticle albumin/rapamycin portion and using quantified albumin species fractions in the nanoparticle coating as suitability indicators, with specified weight-percentage ranges for either albumin polymers or albumin monomers.
Suitability assessment using albumin polymer fraction in nanoparticle coating
A method of assessing suitability of a pharmaceutical composition for medical use in a human individual, comprising separating nanoparticles comprising rapamycin coated with a coating comprising albumin from a non-nanoparticle portion comprising albumin and rapamycin, measuring a weight percentage of albumin in the form of albumin polymers in the coating of the separated nanoparticles among the total albumin in the coating of the separated nanoparticles, and assessing suitability when the albumin polymer weight percentage among total albumin is from about 15% to about 40%.
Suitability assessment using albumin monomer fraction in nanoparticle coating
A method of assessing suitability of a pharmaceutical composition for medical use in a human individual, comprising separating nanoparticles comprising rapamycin coated with a coating comprising albumin from a non-nanoparticle portion comprising albumin and rapamycin, measuring a weight percentage of albumin in the form of albumin monomers in the coating of the separated nanoparticles among the total albumin in the coating of the separated nanoparticles, and assessing suitability when the albumin monomer weight percentage among total albumin is from about 40% to about 60%.
Across the independent claims, suitability for medical use is determined by separating nanoparticles from a non-nanoparticle albumin/rapamycin portion and then quantifying albumin species within the albumin coating of the separated rapamycin-coated nanoparticles, either albumin polymers (about 15% to about 40%) or albumin monomers (about 40% to about 60%).
Stated Advantages
Provides an indicator of suitability for medical use based on quantified albumin polymer or albumin monomer weight percentages in the nanoparticle coating.
Faster dissolution and suspension.
Improved rapamycin stability.
Improved filterability.
Enables validating commercial batches by sampling and assessing suitability according to the described method.
Documented Applications
Assessing suitability of a pharmaceutical composition for medical use in a human individual that comprises rapamycin coated albumin nanoparticles and a non-nanoparticle albumin/rapamycin portion.
Validating and releasing commercial batches for medical use by sampling and assessing suitability using albumin monomer, polymer, and oligomer fractions and nanoparticle characterization.
Medical use in a human individual of a pharmaceutical composition comprising rapamycin-coated albumin nanoparticles plus a non-nanoparticle portion comprising albumin and rapamycin, where suitability is assessed using the claimed albumin species indicators.
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