Interested in licensing this patent?
MTEC can help explore whether this patent might be available for licensing for your application.
Publication Number
US-10682412-B2
Publication Date
2020-06-16
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 concerns tricalcium phosphate (TCP) particles whose surface is coated fully or partially with a biocompatible matrix composition. The matrix composition includes a biodegradable polymer, a first lipid comprising a sterol, a second lipid comprising at least one phospholipid having hydrocarbon chains of at least 14 carbons, and a pharmaceutical active agent.
A key aspect of the matrix composition is that it is lipid saturated and has a multilayered structural arrangement in which the biodegradable polymer and lipids are ordered in layers. The coated TCP particles are configured so that, when maintained in an aqueous environment, the multilayered lipid-saturated matrix provides sustained release of the pharmaceutical active agent.
The disclosed configurations further support relationships between matrix composition and delivery behavior, including sustained release kinetics and formation of vesicles, together with structural ordering and coating stability observations. The document also ties the system to use contexts involving bone-related conditions and coated bone particles/implants with sustained release of active agents.
Claims Coverage
Independent claim coverage centers on coated tricalcium phosphate particles with a lipid-saturated multilayer polymer/lipid matrix that provides sustained release of a pharmaceutical active agent in an aqueous environment. The independent claim set provided here includes one independent claim, with dependent refinements captured as main inventive features tied to composition constraints and added components.
Lipid-saturated multilayer matrix coating for sustained release
Tricalcium phosphate (TCP) particles having their surface coated fully or partially with a biocompatible matrix composition comprising a biodegradable polymer, a first lipid comprising a sterol, a second lipid comprising at least one phospholipid having hydrocarbon chains of at least 14 carbons, and a pharmaceutical active agent; wherein the matrix composition is lipid saturated, has a multilayered structural in which the biodegradable polymer and lipids are ordered in layers, and provides sustained release of the pharmaceutical active agent when maintained in an aqueous environment.
Biodegradable polymer selected as PLA, PGA, or PLGA
The matrix composition includes a biodegradable polyester selected from PLA, PGA and PLGA.
Total lipids to biodegradable polymer weight ratio constraint
The coated particles have a total lipids to biodegradable polymer weight ratio between 1.5:1 and 9:1 inclusive.
Cholesterol content range within lipid content
The matrix composition includes cholesterol having a cholesterol content between 10–50 percent of the total weight of the lipid content in the matrix composition.
Pharmaceutical active agent selection set
The matrix composition includes multiple pharmaceutical active agents selected from antibiotics, antifungals, non-steroidal anti-inflammatory drugs (NSAIDs), steroids, anti-cancer agents, osteogenic factors, and bone resorption inhibitors.
Targeting moiety interacting with selected target molecules
The matrix composition further contains a targeting moiety able to interact with a target molecule selected from collagen, fibrin, or heparin.
Across the provided claim set, the core inventive concept is a lipid-saturated, multilayered biodegradable polymer/lipid matrix coating on TCP particles that yields sustained release in aqueous environments, further refined by specific polymer selection, lipid-to-polymer and cholesterol content constraints, expanded active-agent selection, and inclusion of a targeting moiety for specified target molecules.
Stated Advantages
Provides sustained release of the pharmaceutical active agent when maintained in an aqueous environment.
Provides a lipid-saturated matrix having an ordered multilayer structure in which the biodegradable polymer and lipids are ordered in layers.
Supports homogeneous, water-resistant ordered structures formed with substantially water-free processing.
Documented Applications
Coating of bone filler particles with the lipid-saturated biodegradable polymer/lipid matrix to deliver a pharmaceutical active agent via sustained release in an aqueous environment.
Coating medical implant materials with the matrix composition for sustained release of a pharmaceutical active agent.
Formulation of microspheres or implant-associated dosage forms using the biodegradable polymer/lipid multilayer matrix containing a pharmaceutical active agent.
Targeted delivery configurations using a targeting moiety able to interact with collagen, fibrin, or heparin.
Periodontitis.
Bone infection/bone recovery applications.
Interested in licensing this patent?