Methods and compositions for the delivery of biologically active agents
Inventors
Esfand, Roseita • Santerre, Paul J. • Yang, Meilin
Assignees
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Publication Number
US-8574604-B2
Publication Date
2013-11-05
Expiration Date
Abstract
The invention features polymers noncovalently complexed with a biologically active agent. The polymer complexes include at least one shielding moiety covalently tethered to at least one complexing moiety, which is complexed with at least one biologically active agent.
Core Innovation
The disclosure describes polymer complexes for sustained delivery in which a complexing moiety on an oligomeric segment covalently bears a shielding moiety, including a polyfluoroorgano group. The polymer has a structural formula in which LINK A is an organic moiety comprising tri-hydroxymethyl aminoethane (Tris), and the oligomeric segment is defined as oligo, with a terminal group (T) included in the polymer structure.
Biologically active agents are complexed to LINK A without chemically modifying the biologically active agent, with at least one Bio complexed via hydrogen bonding interactions to at least one LINK A. The polymer complexes are characterized as using non-covalent and coordination interactions, including hydrogen bonding and ionic interactions, as well as inclusion/clathration and van der Waals interactions where applicable.
The approach is positioned to reduce phase separation and maintain drug structural integrity while providing controlled release. The disclosure further states that the shielding moiety and complexing moiety arrangement enables broad composition scope, including selection of biologically active agent classes and suitable polymer/admixture composition choices.
Claims Coverage
The independent claim is directed to a specific polymer structure featuring a polyfluoroorgano group and Tris (LINK A) complexing moieties, with Bio hydrogen-bond complexed to LINK A. Dependent claims refine the structural and compositional scope and extend coverage to release and performance constraints.
Hydrogen-bond complexed Tris LINK A with polyfluoroorgano polymer structure
A polymer having a polyfluoroorgano group (FT) and LINK A moieties, where at least one Bio is complexed via hydrogen bonding interactions to at least one LINK A, each LINK A being an organic moiety comprising tri-hydroxymethyl aminoethane (Tris), and where each Bio is selected from a specified group of biologically active agent classes.
Tris-based complexing moiety on an oligomeric segment with terminal group
The polymer is defined by a structural formula including an oligomeric segment (oligo) and a terminal group (T), with indices a, b, c, d, and e constrained as described in the claim, and with LINK A comprising Tris as the complexing moiety.
Polyfluoroorgano group loading within a specified range
FT is present in the polymer in an amount comprising from about 0.01 to 5 weight % of the polymer.
Oligomeric segment molecular weight constraint
The oligomeric segment has an absolute molecular weight of less than about 10 kDa.
Non-covalent complexation of biologically active agent classes without chemical modification
Each biologically active agent (Bio) is capable of being complexed to LINK A, and the claim framework ties Bio to complexation via hydrogen bonding interactions to LINK A for the selected Bio classes.
Release performance threshold for biologically active agent
80% of the biologically active agent is released within 2 years in the context of the controlled release article described in the dependent claim.
Overall claim coverage centers on a polyfluoroorgano polymer architecture bearing Tris-based LINK A complexing moieties on an oligomeric segment, with at least one biologically active agent hydrogen-bond complexed to LINK A. Dependent claims further constrain polyfluoroorgano loading and oligomer molecular weight and include release performance thresholds, while the independent claim defines the Bio class scope.
Stated Advantages
Enables complexation of biologically active agents via hydrogen bonding interactions to LINK A.
Reduces phase separation.
Maintains drug structural integrity.
Provides controlled/sustained release performance, including an example threshold such as 80% release within 2 years.
Documented Applications
Implantable medical devices, including stents/catheters/valves and related surface coatings, for sustained delivery of biologically active agents.
Anti-inflammatory uses, including inflammation reduction.
Anti-proliferative/restenosis uses, including proliferation control and restenosis reduction.
Analgesic and anesthetic uses, including pain reduction.
Anti-microbial coating uses, including antimicrobials.
Pest control using pesticides/herbicides.
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