Sustained-release drug carrier composition
Inventors
Emanuel, Noam • Neuman, Moshe • Barak, Shlomo
Assignees
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Publication Number
US-8992979-B2
Publication Date
2015-03-31
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 medical device having a substrate with a biocompatible coating deposited on at least a fraction of the substrate. The coating comprises a non-liposomal matrix composition that contains a biocompatible non-biodegradable polymer non-covalently associated with a first lipid comprising at least one sterol having a polar group, and a second lipid comprising at least one phospholipid with hydrocarbon chains of at least 14 carbons, wherein the non-biodegradable polymer is not bonded to the second lipid.
The coating further comprises at least one pharmaceutically active agent. The matrix composition is lipid saturated and, when maintained in an aqueous environment, provides zero-order release of at least 40% of the pharmaceutically active agent. The matrix is described as a substantially water-free, homogeneous, water-resistant implantable composition formed with lipid saturation.
The description further states that release is tied to the polymer-lipid ratio and lipid fluidity, with sustained or controlled release over days to months and a shift toward zero-order kinetics after a lag. The document also describes embodiments as implants, coatings, and microspheres.
Claims Coverage
The independent claim set is centered on one independent claim that defines a lipid-saturated, non-liposomal coated medical device matrix providing zero-order release in aqueous environments. Dependent claims refine the independent claim with quantitative composition constraints and additional limitations, including release fraction ranges and processing and use-case constraints.
Lipid-saturated non-liposomal polymer–sterol–phospholipid matrix coating for a substrate
A medical device having a substrate with a biocompatible coating deposited on at least a fraction of the substrate, where the biocompatible coating comprises a non-liposomal matrix composition including a biocompatible non-biodegradable polymer non-covalently associated with a first lipid comprising at least one sterol having a polar group, and a second lipid comprising at least one phospholipid having hydrocarbon chains of at least 14 carbons, wherein the non-biodegradable polymer is not bonded to the second lipid, and at least one pharmaceutically active agent.
Zero-order release of at least 40% of the pharmaceutically active agent in aqueous environment
Wherein the matrix composition is lipid saturated and when maintained in an aqueous environment provides zero-order release of at least 40% of the pharmaceutically active agent.
Coverage is anchored by a single independent claim defining a non-liposomal, lipid-saturated matrix coating that non-covalently associates a non-biodegradable polymer with a sterol-containing first lipid and includes a phospholipid with hydrocarbon chains of at least 14 carbons, with at least one pharmaceutically active agent and zero-order release of at least 40% in an aqueous environment.
Stated Advantages
Provides zero-order release of at least 40% of the pharmaceutically active agent when maintained in an aqueous environment.
Matrix is lipid saturated and described as substantially water-free, homogeneous, and water-resistant.
Documented Applications
Treating periodontitis by applying the medical device to a bone loss site in a subject requiring treatment.
Bone-recovery application areas described in the document include periodontitis, orthopedic/bone augmentation, and osteomyelitis.
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