Nanosphere size control by varying the ratio of copolymer blends
AssigneeRutgers, The State University of New Jersey
InventorsJoachim B. Kohn, Mariana Reis Nogueira de Lima
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Abstract
Nanosphere composition containing a mixture of a triblock oligomer and a diblock oligomer for the delivery of an active agent. Also disclosed are methods of preparing the nanospheres and methods of delivering an active agent enclosed in the nanospheres.
Claims21
A nanosphere composition for delivery of an active agent, comprising a distribution of nanospheres with essentially the same hydrodynamic Z-average diameter in a pharmaceutically acceptable carrier, said nansospheres consisting essentially of a mixture of the same triblock oligomer and the same diblock oligomer, wherein:
- the triblock oligomer consists of a single A-B-A structure and the diblock oligomer consists of a single A-B-H structure, wherein A and B in the diblock oligomer are identical to A and B in the triblock oligomer;
- wherein the B block is hydrophobic with repeating units having the structure according to Formula I:
- wherein
- Z is an integer, between 2 and about 100, inclusive, that provides the B block with a weight-average molecular weight between about 1000 and about 30,000 g/mol;
- R1 is CH═CH or (CH2)n wherein n is from 0 to 18, inclusive;
- R2 is straight or branched alkyl and alkylaryl groups containing up to 18 carbon atoms;
- R3 is selected from the group consisting of a bond or straight and branched alkyl and alkylaryl groups containing up to 18 carbon atoms, wherein R2 and R3 together contain more than 6 carbons, provided that when R2 is (CH2)3CH3, R3 is not (CH2)4;
- wherein the A block is a poly(alkylene oxide) having the structure:
- R4 for each A and within each A is independently selected from the group consisting of hydrogen and lower alkyl groups containing from one to four carbon atoms;
- R5 for each A and within each A is independently selected from the group consisting of hydrogen and lower alkyl groups containing from one to four carbon atoms;
- m for each A is independently selected to provide a molecular weight for each A between about 1000 and about 15,000 g/mol.
A method of preparing nanoparticles having a predetermined hydrodynamic Z-average diameter as measured by DLS, consisting essentially of triblock oligomers having the same A-B-A structure and diblock oligomers having the same A-B-H structure, wherein A and B in the diblock oligomer are identical to A and B in the triblock oligomer, the method comprising:
- (a) blending separate quantities of the triblock and diblock oligomers, wherein the respective quantities are selected to provide the nanoparticles having a predetermined hydrodynamic Z-average diameter,
- (b) dissolving the blended oligomers in an organic solvent in which the oligomers are soluble to provide an organic solution of the diblock and triblock oligomers, and
- (c) adding the organic solution to an aqueous solution to form an aqueous suspension of the nanoparticles having a predetermined hydrodynamic Z-average diameter;
- wherein the B block is hydrophobic with repeating units having the structure according to Formula I:
- wherein
- Z is an integer, between 2 and about 100, inclusive, that provides the B block with a weight-average molecular weight between about 1000 and about 30,000 g/mol;
- R1 is CH═CH or (CH2)n wherein n is from 0 to 18, inclusive;
- R2 is straight or branched alkyl and alkylaryl groups containing up to 18 carbon atoms;
- R3 is selected from the group consisting of a bond or straight and branched alkyl and alkylaryl groups containing up to 18 carbon atoms, wherein R2 and R3 together contain more than 6 carbons;
- wherein the A block is a poly(alkylene oxide) having the structure:
- R4 for each A and within each A is independently selected from the group consisting of hydrogen and lower alkyl groups containing from one to four carbon atoms;
- R5 for each A and within each A is independently selected from the group consisting of hydrogen and lower alkyl groups containing from one to four carbon atoms;
- m for each A is independently selected to provide a molecular weight for each A between about 1000 and about 15,000 g/mol.
21-24. (canceled)
Dependencies are inferred from the claim text.