Biodegradable block copolymer drug delivery composition
Inventors
Roberge, Christophe • RECH, Anthony • CROS, Jean-Manuel • ABBASSI, Myriam • LÓPEZ-NORIEGA, Adolfo • PEBREL, Lea • Petit, Audrey • SERINDOUX, Juliette
Assignees
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Publication Number
US-11666527-B2
Publication Date
2023-06-06
Expiration Date
Abstract
Provided is a biodegradable drug delivery composition comprising: (i) a mixture of at least three different block copolymers, wherein each block copolymer is: (a) a biodegradable triblock copolymer having the formula: Av-Bw-Ax wherein A is a polyester and B is polyethylene glycol and v and x are from 1 to 3,000 and w is from 3 to 300 and v=x or v≠x; or (b) a biodegradable diblock copolymer having the formula: Cy-Az wherein A is a polyester and C is an end-capped polyethylene glycol and y=2 to 250 and z=1 to 3,000; and wherein the mixture comprises at least one (a) and at least one (b); and the weight ratio between (a) and (b) is 1:19 to 5:1; and for at least one of the copolymers according to (a) or (b) A is poly(lactic-co-glycolic acid) (PLGA); and (ii) at least one pharmaceutically active ingredient.
Core Innovation
The invention relates to an injectable biodegradable drug delivery composition comprising a mixture of at least three different block copolymers and at least one pharmaceutically active ingredient. The block copolymers include biodegradable triblock copolymers A(v)-B(w)-A(x) and biodegradable diblock copolymers C(y)-A(z), wherein A is a polyester, B is polyethylene glycol, and C is an end-capped polyethylene glycol.
The mixture further requires that the weight ratio of the sum of the biodegradable triblock copolymers to the sum of the biodegradable diblock copolymers is 1:19 to 5:1, and for at least one of the copolymers A is poly(lactic-co-glycolic acid) (PLGA). The composition is designed so that the release kinetics of at least one active ingredient can be modulated while maintaining injectability and/or viscosity before injection and/or depot robustness after injection.
The described approach is presented as a comparison against a composition having a single biodegradable triblock copolymer and a single biodegradable diblock copolymer. Example formulations are described for meloxicam and acetaminophen showing altered in vitro release profiles, including changes made by substitution of an additional biodegradable block copolymer without significant changes to injectability or dynamic viscosity.
Claims Coverage
The independent claim coverage describes one main inventive concept with three inventive features: an injectable biodegradable block-copolymer mixture, a triblock-to-diblock weight-ratio constraint, and release-kinetics modulation while preserving injectability, viscosity, and/or depot robustness relative to a single-triblock/single-diblock composition.
Injectable biodegradable mixture of triblock and diblock block copolymers
An injectable biodegradable drug delivery composition comprising a mixture of at least three different block copolymers, including biodegradable triblock copolymers A(v)-B(w)-A(x) and biodegradable diblock copolymers C(y)-A(z), wherein the mixture comprises at least one triblock and at least one diblock.
Triblock/diblock weight ratio for release-kinetics modulation
The composition wherein the weight ratio of the sum of the biodegradable triblock copolymers to the sum of the biodegradable diblock copolymers is 1:19 to 5:1, and wherein for at least one copolymer A is poly(lactic-co-glycolic acid) (PLGA).
Release kinetics modulation without harming injectability, viscosity, or depot robustness
An injectable biodegradable drug delivery composition wherein release kinetics of at least one pharmaceutically active ingredient can be modulated without adversely affecting injectability and/or viscosity before injection and/or depot robustness after injection, compared to a composition having a single biodegradable triblock and a single biodegradable diblock.
Overall, the claims define an injectable biodegradable composition built from a triblock/diblock block-copolymer mixture with a specified triblock-to-diblock weight ratio and at least one PLGA-containing block, where release kinetics are modulated while preserving injectability, viscosity before injection, and/or depot robustness after injection relative to single-triblock/single-diblock controls.
Stated Advantages
Modulates release kinetics of at least one active ingredient without adversely affecting injectability and/or viscosity before injection.
Modulates release kinetics of at least one active ingredient without adversely affecting depot robustness after injection.
Provides improved release-kinetics tunability compared to a composition having a single biodegradable triblock and a single biodegradable diblock.
Documented Applications
Injectable biodegradable drug delivery compositions suitable for parenteral administration.
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