Injectable and biodegradable polymer formulations for controlled release of bioligic agents

A bioactive agent and polymer technology, applied in the field of injectable polymer preparations, can solve the problems of bioactive agent delivery and inability of drops to penetrate significantly

Pending Publication Date: 2019-11-19
WL GORE & ASSOC INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Topically applied treatments such as eye drops are ineffective in treating disorders of the posterior segment of the eye because the drops do not significantly penetrate the eye and deliver bioactive agents to the target site
Injection directly into the eye using conventional needles and syringes to deliver biologics has been successful, but requires specialized training and/or multiple injections to complete treatment

Method used

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  • Injectable and biodegradable polymer formulations for controlled release of bioligic agents
  • Injectable and biodegradable polymer formulations for controlled release of bioligic agents
  • Injectable and biodegradable polymer formulations for controlled release of bioligic agents

Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0055] Example 1

[0056] This example describes the copolymer L-PLA:TMC in a weight ratio of 55:45. Table 1 shows characterization data for the compositions of this example.

[0057] Intrinsic viscosity (IV) was measured using a Cannon MiniPV-HX automatic viscometer with hexafluoroisopropanol (HFIP) as the extraction solvent. For this example, IV(HFIP) = 1.07 dL / g.

Example Embodiment

[0058] Example 2

[0059] This example describes the copolymer L-PLA:TMC in a weight ratio of 55:45. Table 1 shows characterization data for the compositions of this example.

[0060] Intrinsic viscosity (IV) was measured using a Cannon MiniPV-HX automatic viscometer with hexafluoroisopropanol (HFIP) as the extraction solvent. For this example, IV(HFIP) = 1.36 dL / g.

Example Embodiment

[0061] Example 3

[0062] This example describes the copolymer D,L-PLA:TMC in a weight ratio of 50:50. Table 1 shows characterization data for the compositions of this example.

[0063] Intrinsic viscosity was measured using a Cannon MiniPV-HX automatic viscometer with chloroform (CHCl3) as the extraction solvent. For this example, IV(CHCl3) = 0.933 dL / g and the glass transition temperature of the polymer was determined to be 7.2°C.

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Abstract

The present disclosure is directed to injectable formulations that include biodegradable polymers based on trimethylene carbonate (TMC) with mole fractions of polylactic acid (PLA) and/or polyglycolicacid (PGA) that are used to deliver a bioactive agent to a targeted site. Excipients such as polyethylene glycol (PEG) may be added to the formulations to reduce the injection force and/or to modulate the release of the bioactive agent. Suitable biodegradable polymers for use in the injectable formulations include D, L-PLA:TMC, D-PLA:TMC, L-PLA:TMC, TMC:PLA:PGA and variations thereof. Additionally, copolymers of TMC and PLA and terpolymers of TMC:PLA:PGA may be formed into nanoparticles and delivered to the target site with an injectable crosslinkable polyethylene glycol system. In at least one embodiment, the injectable formulations are used to treat ocular diseases.

Description

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Claims

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Application Information

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Owner WL GORE & ASSOC INC
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