Carmustine formulation
Inventors
GONDALIYA, Deepak Pragjibhai • PATEL, Hiren Pravinbhai • PATEL, Haresh Ishwarbhai • Gurjar, Mukund Keshav
Assignees
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Publication Number
US-12427127-B2
Publication Date
2025-09-30
Expiration Date
Abstract
The present invention relates to a composition comprising nitrosourea and pharmaceutically acceptable excipients. In particular, the present invention relates to novel drug delivery systems of carmustine such as nano-suspension and micro-emulsion and its use for the treatment of cancer by intravenous administration. Also provided are methods for preparation of such novel drug delivery systems.
Core Innovation
The patent describes a carmustine drug composition for intravenous cancer treatment that uses a nano-suspension formulation and is distinguished from conventional lyophilized BiCNU (carmustine for injection). The background describes conventional lyophilized BiCNU as having poor water solubility and hydrolysis, which is associated with toxicity and low selectivity.
The core formulation contains carmustine, a combination of phosphatidylcholine and sodium cholesteryl sulfate, poly(lactic-co-glycolic acid) (PLGA), sucrose, and water, where the ratio of carmustine to PLGA ranges from 1:3 to 1:6 (w/w). The composition is characterized as a nano-suspension intended for intravenous administration in cancer therapy.
The disclosed approach further defines component selection and composition concepts for creating stable nano-suspensions, including use of phosphatidylcholine with sodium cholesteryl sulfate and inclusion of sucrose with water. The document reports stability at 2–8°C for at least 3 months with impurity and assay limits, and provides example formulations and referenced experimental outcomes versus a BiCNU reference product, including tumor regression and reduced acute mortality in animal studies.
Claims Coverage
The independent claim covers one core nano-suspension drug composition defined by specific weight-percent ranges and a defined carmustine-to-PLGA ratio, and it is further refined by dependent claims directed to a lyophilized powder form and to particular component selection and a specific treatment method for enumerated diseases. Overall, the claim set is centered on carmustine nano-suspension delivery using phosphatidylcholine plus sodium cholesteryl sulfate with PLGA and sucrose in water.
Carmustine nano-suspension with phosphatidylcholine and sodium cholesteryl sulfate, PLGA, sucrose, and water
A drug composition comprising 0.1 wt % to 50 wt % of carmustine; 1 wt % to 70 wt % of a combination of phosphatidylcholine and sodium cholesteryl sulfate; 1 wt % to 60 wt % of PLGA; sucrose and water, wherein the ratio of carmustine to PLGA ranges from 1:3 to 1:6 (w/w) and the composition is a nano-suspension.
Lyophilized powder form of the nano-suspension composition
The composition of claim 1 wherein the drug composition is a lyophilized powder obtained by lyophilizing the drug composition of claim 1.
Soybean phosphatidylcholine selection
The composition of claim 1 wherein the phosphatidylcholine component is soybean phosphatidylcholine.
Subrange constraints for carmustine and the phosphatidylcholine/sodium cholesteryl sulfate combination
The composition of claim 1 containing carmustine in a specified weight-percent range and containing 1 wt % to 40 wt % of the phosphatidylcholine and sodium cholesteryl sulfate combination.
Parenteral treatment using lyophilized powder with a selected carrier for specific malignancies
A method for treating brain tumors, brain metastases, meningeal leukemia, malignant lymphoma, or multiple myeloma by combining an effective amount of a lyophilized powder with a selected carrier and parenterally administering the resulting combination to a patient.
The claim coverage focuses on a nano-suspension drug composition containing carmustine with a phosphatidylcholine plus sodium cholesteryl sulfate combination, PLGA, sucrose, and water with a defined carmustine-to-PLGA ratio. Dependent claims refine the composition to a lyophilized powder form, specify soybean phosphatidylcholine, narrow subranges for carmustine and the phosphatidylcholine/sodium cholesteryl sulfate combination, and recite a treatment method for enumerated brain and hematologic malignancies using the lyophilized powder with a selected carrier and parenteral administration.
Stated Advantages
Reduced acute mortality and tumor regression in animal studies versus a BiCNU reference product.
Improved suitability relative to conventional lyophilized BiCNU described as addressing poor water solubility and hydrolysis that are associated with toxicity and low selectivity.
Stability at 2–8°C for at least 3 months with impurity and assay limits.
Documented Applications
Intravenous cancer treatment using carmustine nano-suspension for brain tumors, brain metastases, meningeal leukemia, malignant lymphoma, and multiple myeloma.
Treatment method based on combining an effective amount of a lyophilized powder with a selected carrier followed by parenteral administration to a patient with brain tumors, brain metastases, meningeal leukemia, malignant lymphoma, or multiple myeloma.
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