CROSSLINKED POLYMER NANO-ASSEMBLIES AND USES THEREOF
First Claim
1. A nano-assembly for controlled delivery of a therapeutic or diagnostic agent to a biological site, comprising:
- a water-soluble polymer host comprising a crosslinked network of polymer molecules; and
a guest molecule comprising a therapeutic, diagnostic, or imaging agent non-covalently associated with the polymer host, wherein the therapeutic or diagnostic agent is releasable upon partial or complete de-crosslinking of the crosslinked network of polymer molecules at or near the biological site.
4 Assignments
0 Petitions
Accused Products
Abstract
The invention provides a novel system of nano-assemblies and related method for delivery of therapeutic, diagnostic or imaging agent to biological sites. The compositions and methods of the invention enable the syntheses of novel polymeric nano-assemblies (nanoparticles) under non-emulsion conditions with the incorporation of hydrophobic guest molecules. The versatilities and advantages of the polymer nanoparticles of the invention include: (i) the guest molecules (e.g., drug molecules) can be readily incorporated non-covalently within the nanoparticles; (ii) the surface of the nanoparticles are functionalizable; (iii) the non-covalently encapsulated guest molecule (payload) can be released in response to a biologically relevant stimulus at the target site; (iv) the payload is held by the polymeric nanoparticle before being internalized in cells and can be released within the cellular interiors; (v) encapsulating lipophilic small molecules within its crosslinked interiors and binding proteins on its surface through electrostatic interactions; (vi) facile synthetic methods for ligand functionalization that can be utilized to decorate nanogels with cell targeting ligands that facilitate receptor-dependent cellular uptake, and (vii) the payload release kinetics is tunable and controllable.
9 Citations
91 Claims
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1. A nano-assembly for controlled delivery of a therapeutic or diagnostic agent to a biological site, comprising:
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a water-soluble polymer host comprising a crosslinked network of polymer molecules; and a guest molecule comprising a therapeutic, diagnostic, or imaging agent non-covalently associated with the polymer host, wherein the therapeutic or diagnostic agent is releasable upon partial or complete de-crosslinking of the crosslinked network of polymer molecules at or near the biological site. - View Dependent Claims (4, 5, 8, 10, 16, 19, 22, 24, 26, 28, 30, 31, 35, 36, 40, 41, 47, 48, 49)
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2. (canceled)
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3. (canceled)
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6. (canceled)
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7. (canceled)
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9. (canceled)
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11-15. -15. (canceled)
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20. (canceled)
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21. (canceled)
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23. (canceled)
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25. (canceled)
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27. (canceled)
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29. (canceled)
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32-34. -34. (canceled)
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37-39. -39. (canceled)
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42-46. -46. (canceled)
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50-56. -56. (canceled)
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57. A nano-assembly for controlled concurrent delivery of small molecule and non-small molecule therapeutic, diagnostic or imaging agents to a biological site, comprising:
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a water-soluble polymer host comprising a crosslinked network of polymer molecules; a guest small molecule therapeutic, diagnostic or imaging agent non-covalently associated within the crosslinked network of polymer molecules, wherein the guest small molecule therapeutic, diagnostic or imaging agent is releasable upon partial or complete de-crosslinking of the crosslinked network of polymer molecules at or near the biological site; and a guest non-small molecule therapeutic, diagnostic or imaging agent covalently linked to or non-covalently associated with the polymer host, wherein the guest non-small molecule therapeutic, diagnostic or imaging agent is releasable at or near the biological site.
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58-89. -89. (canceled)
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90. A method for delivering a therapeutic, diagnostic or imaging agent to a biological site, comprising:
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providing a nano-assembly, comprising; a water-soluble polymer host comprising a crosslinked network of polymer molecules; and a guest molecule comprising a therapeutic, diagnostic or imaging agent non-covalently associated with the polymer host, wherein the therapeutic, diagnostic or imaging agent is releasable upon partial or complete de-crosslinking of the crosslinked network of polymer molecules at or near the biological site; transporting the nano-assembly to the biological site; and causing at least partial de-crosslinking of the crosslinked network of polymer molecules, thereby releasing the therapeutic, diagnostic or imaging agent at or near the biological site.
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91-141. -141. (canceled)
Specification