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Publication Number
US-10105443-B2
Publication Date
2018-10-23
Expiration Date
Abstract
The present invention provides compositions for extended release of an active ingredient, comprising a lipid-saturated matrix formed from a biodegradable polymer. The present invention also provides methods of producing the matrix compositions and methods for using the matrix compositions to provide controlled release of an active ingredient in the body of a subject in need thereof.
Core Innovation
The invention provides lipid-saturated, water-resistant sustained/controlled release matrices for local delivery of an antibiotic agent. The matrices are formed from a biodegradable polymer and associated sterol-containing lipid and phospholipid components to create an ordered multilayer structure that sustains release when maintained in an aqueous environment.
In the disclosed osteomyelitis treatment method, a substrate with at least partially coated surface is administered at or near the site of osteomyelitis. The coated surface includes the matrix composition comprising a biodegradable polymer, a sterol-containing lipid, a fatty-chain-length phospholipid, and an antibiotic agent, and the ordered multilayer structure comprises layers in which the biodegradable polymer and lipid are ordered.
The described compositions are lipid saturated and comprise at least 50% (w/w) lipids. The document further describes homogeneous lipid-saturated biodegradable polymer matrices and implant or microsphere formats, together with long-term release and structure evidence supporting sustained release in aqueous environment.
Claims Coverage
The disclosed claim coverage centers on one independent claim directed to treating osteomyelitis using an administered substrate with a lipid-saturated ordered multilayer antibiotic-release matrix. Dependent claims add quantitative constraints on release extent and time window, composition fractions and ratios, polymer selection, and substrate materials.
Lipid-saturated ordered multilayer antibiotic matrix on a coated substrate
A method of treating osteomyelitis comprising administering at or near the site a substrate whose surface is at least partially coated with a matrix composition for sustained antibiotic release, the matrix composition comprising a biodegradable polymer, a first lipid comprising a sterol, a second lipid comprising at least one phospholipid having fatty acid moieties of at least 14 carbons, and an antibiotic agent; wherein the matrix composition is lipid saturated, comprises at least 50% (w/w) lipids, has an ordered multilayer structure with biodegradable polymer and lipid ordered in layers, and when maintained in an aqueous environment provides sustained release of the antibiotic agent.
Sustained release extent and time window
The method wherein 90% of the antibiotic agent is released during a period of between 4 days and 6 months.
Total lipid to biodegradable polymer weight ratio
The method wherein the weight ratio of total lipids to the biodegradable polymer in the matrix composition is between 1.5:1 and 9:1 inclusive.
Phosphatidylcholine fraction of total lipid
The method wherein the phosphatidylcholine constitutes at least 50% (w/w) of the total lipid content of the matrix composition.
Biodegradable polymer selected from specified polyesters
The method wherein the biodegradable polymer is a biodegradable polyester selected from the group consisting of PLA, PGA and PLGA.
Substrate selected from specified coating base materials
The method wherein the substrate is selected from the group consisting of hydroxyapatite, ceramic material, gelatin, bone filler particles, polymeric implants, collagen and non-collagen membranes, orthopedic cements and sponges.
Across the independent claim and its dependents, the core inventive coverage centers on a lipid-saturated, ordered multilayer matrix containing a biodegradable polymer, a sterol-containing lipid, and a long-chain phospholipid, combined with an antibiotic agent, applied as a coated substrate at the osteomyelitis site to provide sustained antibiotic release in aqueous environment. Dependent features further constrain release extent/time, lipid/polymer weight ratio, phosphatidylcholine fraction, biodegradable polyester selection, and eligible substrate materials.
Stated Advantages
Provides sustained release of the antibiotic agent when the matrix composition is maintained in an aqueous environment.
Lipid saturated matrix with at least 50% (w/w) lipids and ordered multilayer structure supports extended in vivo release.
Ordered multilayer structure in which biodegradable polymer and lipid are ordered in layers to support sustained release.
Documented Applications
Treating osteomyelitis by administering at or near the site a substrate coated with a matrix composition for sustained antibiotic release.
Use in preclinical/clinical testing contexts for osteomyelitis with antibiotic and/or NSAID-loaded implants.
Use in osteomyelitis and periodontitis contexts, including implants carrying antibiotic and/or NSAID components.
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