Method for morselizing and/or targeting pharmaceutically active principles to synovial tissue

Inventors

Gaudriault, Georges • Grizot, Sylvestre • HURTIG, Mark • Shive, Matthew

Assignees

MedinCell SA

Abstract

A method of targeting to the synovial tissue biodegradable drug delivery compositions or morselizing biodegradable drug delivery compositions are described. The biodegradable drug composition comprises a triblock copolymer containing a polyester and a polyethylene glycol and a diblock copolymer containing a polyester and an end-capped polyethylene glycol, as well as at least one pharmaceutically active principle is disclosed.

Core Innovation

The invention relates to methods to morselize a biodegradable drug delivery composition comprising at least one pharmaceutically active principle. The method forms a biodegradable drug composition by combining a biodegradable triblock copolymer of PLA-PEG-PLA and a biodegradable diblock copolymer of mPEG-PLA or analogous end-capped PEG-PLA with at least one pharmaceutically active principle. The triblock and diblock copolymers are defined by repeat-unit ranges, and the polyethylene glycol chain in the triblock and/or diblock copolymer is specified as 2 kDa.

The invention further administers the formulated biodegradable drug delivery composition in at least one joint of a patient such that it is contained within the articulating joint capsule. In the disclosed approach, intra-articular administration is described as an injectable liquid that becomes an in situ hardened implant, or as spatial or rod implant forms that undergo mechanical-challenge-driven fragmentation. The hardened implant is described as being morselized into smaller pieces.

The disclosed compositions are described as targeting synovial and other joint tissues, including articular cartilage, ligaments, tendons, and meniscus. The patent text indicates that the formulation and PEG chain size can influence observed morselization and distribution. The description includes example results showing celecoxib concentration-time profiles in sheep synovial fluid and synovial tissue, together with qualitative morselization and distribution behavior under different formulation compositions and PEG chain sizes.

Claims Coverage

The independent claim provides two inventive features: specific PLA-PEG-PLA triblock and mPEG-PLA diblock copolymer compositions for morselizing, and intra-articular administration contained within the articulating joint capsule. The dependent claims further refine formulation and administration and add quantitative constraints and representative active principle lists.

Across the independent claim, the core coverage ties morselizing to specific biodegradable PLA-PEG-PLA triblock and mPEG-PLA diblock copolymer structures with defined repeat-unit ranges and a triblock:diblock ratio, combined with at least one pharmaceutically active principle, followed by intra-articular administration contained within the articulating joint capsule.

Stated Advantages

Documented Applications