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Publication Number
US-10463617-B2
Publication Date
2019-11-05
Expiration Date
Abstract
The present invention provides compositions for extended release of one or more active ingredients, comprising a lipid-saturated matrix formed from a non-biodegradable polymer or a block-co-polymers comprising a non-biodegradable polymer and 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 relates to a non-liposomal matrix composition that combines a biocompatible non-biodegradable polymer with a lipid system and at least one pharmaceutically active agent. The lipid system includes a first lipid comprising at least one sterol and a second lipid comprising at least one phospholipid with fatty acid moieties having at least 14 carbons, and the polymer is not covalently bonded to the first and second lipids.
When maintained in an aqueous environment, the matrix composition provides sustained release of the pharmaceutically active agent. The composition is described as lipid-saturated and substantially free from water, supporting lipid saturation and lipid backbone stability, and the sustained release behavior is described as tunable, including sustained/extended controlled release and zero-order kinetics.
The matrix can optionally further include an additional phospholipid selected from phosphatidylserine, phosphatidylglycerol, and phosphatidylinositol, a sphingolipid, PEGylated lipid, tocopherol, physiologically acceptable buffer salts, and/or a targeting moiety. An optional biodegradable polymer is also described, including a biodegradable polymer in the form of a block-co-polymer with the non-biodegradable polymer.
The described embodiments and examples include pharmaceutical compositions, implants, and injectable formulations for delivering NSAIDs and antibiotics, as well as matrix formation and drug release behavior studies, including doxycycline formulations with different phospholipids.
Claims Coverage
The disclosure provides one independent claim directed to a non-liposomal matrix composition. The independent claim includes a polymer/lipid/active-agent construct requiring sustained release in an aqueous environment, supported by the requirement that the polymer is not covalently bonded to the lipids.
Non-liposomal matrix with specified polymer, sterol lipid, and long-chain phospholipid
A non-liposomal matrix composition consisting of a biocompatible non-biodegradable polymer, a first lipid comprising at least one sterol, and a second lipid comprising at least one phospholipid having fatty acid moieties having at least 14 carbons, together with at least one pharmaceutically active agent.
Polymer not covalently bonded to the lipids for aqueous sustained release
The non-biodegradable polymer is not covalently bonded to the first and second lipids, and when maintained in an aqueous environment the matrix composition provides sustained release of the pharmaceutically active agent.
Optional additional lipids, PEGylated lipid, buffer salts, and targeting moiety
The matrix composition optionally includes at least one of an additional phospholipid selected from phosphatidylserine, phosphatidylglycerol, and phosphatidylinositol; a sphingolipid; PEGylated lipid; tocopherol; physiologically acceptable buffer salts; or a targeting moiety.
Optional biodegradable polymer block copolymer
The matrix composition optionally includes at least one biodegradable polymer, wherein the biodegradable polymer is optionally in the form of a block-co-polymer with the non-biodegradable polymer.
Overall, the independent claim centers on a non-liposomal matrix composition defined by a non-biodegradable polymer not covalently bonded to a sterol-containing lipid and a long-chain phospholipid, formulated with a pharmaceutically active agent to provide sustained release in an aqueous environment, with optional additional lipids, PEGylated lipid, buffer salts, targeting moiety, and optional biodegradable polymer block copolymer.
Stated Advantages
Sustained release of the pharmaceutically active agent when maintained in an aqueous environment.
Sustained/extended controlled release behavior, including release performance described as zero-order kinetics.
Lipid saturation and lipid backbone stability.
Documented Applications
Delivering NSAIDs and antibiotics alone or co-administered using pharmaceutical compositions, implants, and injectable formulations.
Treating periodontitis, including chronic periodontitis.
Stimulating bone augmentation.
Reducing orthopedic-surgery complications.
Enhancing surgical regenerative procedures, including periodontal/ridge-sinus augmentation.
Treating osteomyelitis.
Supporting orthopedic bone and soft tissue recovery/homeostasis by sustained drug release and reduced inflammation, infections, and adhesions.
Medical uses for periodontal indications.
Medical uses for orthopedic indications, including bone augmentation and bone infection contexts such as osteomyelitis.
Matrix formation and drug release behavior studies, including doxycycline hyclate (Doxy-H) formulations with different phospholipids.
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