Combinatorial polymeric compositions for drug delivery
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Publication Number
US-8728453-B2
Publication Date
2014-05-20
Expiration Date
Abstract
The present invention is directed towards the synthesis of polymeric drug delivery compositions which would address some of the important and difficult to realize aspects of polymer based drug delivery systems by being, biocompatible, stable, capable of achieving desired drug loading, and safe from accidental release while being non-toxic, easy to fabricate and safe for the environment.
Core Innovation
A combinatorial library of biodegradable polymeric compositions is made by arming or derivatizing an active molecule and optionally a natural product with at least one hydrolysable linker that has at least one reactive end group to form an armed or derivatized active molecule and optionally an armed or derivatized natural product. One or more monomers having at least two polymerizable functionalities are mixed with the armed or derivatized active molecule and optionally the armed or derivatized natural product using predetermined stoichiometry to form mixtures, and the mixtures are co-polymerized to form pools of pre-polymers.
Predetermined stoichiometry of the pre-polymers is then mixed and copolymerized with selected monomers to obtain the polymeric compositions. The polymeric compositions are treated with capping reagents to give a combinatorial library of biodegradable polymeric compositions. The biodegradable polymeric compositions allow a predetermined loading of the active molecule or the armed active molecule by adjusting the quantity of the active molecule or the armed active molecule in the mixture before subjecting the mixture to polymerization.
The active molecule is selected from drugs, nutraceuticals, and imaging agents. The natural product is a naturally occurring plant polyphenol or derivative thereof, and the reactive end groups and functionalities are selected from thiol, allyl, amine, anhydride, azido, carboxy, epoxy, hydroxy, isocyanate, lactone, propargyl, thiocyanate, or vinyl. The approach forms biodegradable polymer matrices in which polymerizable functionality from the armed payload and selected monomers is used to build polymeric compositions and libraries.
Claims Coverage
The provided independent claim sets out a method for making a combinatorial library of biodegradable polymeric compositions with four inventive features: arming or derivatizing payloads with hydrolysable linkers bearing reactive end groups, copolymerizing to form pre-polymers and then final polymeric compositions, capping to obtain the library, and predetermined loading by adjusting payload quantity prior to polymerization. It specifies that active molecules include drugs, nutraceuticals, and imaging agents, that natural products include plant polyphenols or derivatives, and that reactive end groups include a defined set.
Combinatorial library method using arming or derivatization with hydrolysable linkers and capping
A method of making a combinatorial library of biodegradable polymeric compositions by arming or derivatizing an active molecule and optionally a natural product with at least one hydrolysable linker having at least one reactive end group, forming mixtures with monomers having at least two polymerizable functionalities, co-polymerizing to form pools of pre-polymers, mixing and copolymerizing with selected monomers to obtain polymeric compositions, and treating the polymeric compositions with capping reagents to give the combinatorial library.
Predetermined loading by adjusting active molecule quantity before polymerization
The biodegradable polymeric compositions allow a predetermined loading of the active molecule or the armed active molecule by adjusting the quantity of the active molecule or the armed active molecule in the mixture before subjecting the mixture to polymerization.
Payload selection and reactive end group functionality set
The active molecule is selected from drugs, nutraceuticals, and imaging agents; the natural product is a naturally occurring plant polyphenol or derivative thereof; and the reactive end groups and functionalities are selected from thiol, allyl, amine, anhydride, azido, carboxy, epoxy, hydroxy, isocyanate, lactone, propargyl, thiocyanate, or vinyl.
Across the independent claim, the inventive concept is a combinatorial method that produces biodegradable polymeric compositions by arming or derivatizing payloads with hydrolysable linkers bearing reactive end groups, forming pre-polymers via co-polymerization with monomers of at least two polymerizable functionalities and then copolymerizing pre-polymers with selected monomers, followed by capping to yield a library. Predetermined loading is achieved by adjusting payload quantity before polymerization, with payload and reactive end groups restricted to specified categories.
Stated Advantages
Allows a predetermined loading of the active molecule or the armed active molecule by adjusting quantity in the mixture before subjecting the mixture to polymerization.
Documented Applications
No documented applications found
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