Ophthalmic And Otic Compositions Of Facially Amphiphilic Polymers And Oligomers And Uses Thereof

a technology of amphiphilic polymers and compositions, applied in the field of amphiphilic antimicrobial compositions of facially amphiphilic polymers and oligomers, can solve the problems of bacterial drug resistance, determinants, and virtually untreatable current antimicrobial agents, and achieve the effect of treating or preventing

Inactive Publication Date: 2009-04-09
POLYMEDIX
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0036]The present invention is also directed to an otic composition for use in treatment or prevention of a microbial infection in an ear of an animal, wherein the composition comprises an antimicrobial oligomer of Formula I, Formula II, Formula IIa, Formula IV, Formula IVa, Formula IVb, Formula IVc, Formula V, Formula Va, or Formula VI as disclosed herein, or an acceptable salt or solvate thereof, in an amount effective to treat or prevent the infection when the composition is administered to one or more tissues of the ear.

Problems solved by technology

Bacterial drug resistance is a significant current health problem throughout the world.
For example, in some U.S. hospitals, nosocomial pathogens, such as E. faecium and Acinetobacter species, have acquired multiple resistance determinants and are virtually untreatable with current antimicrobial agents.
Moreover, the threat of bio-terrorism has provided a further impetus to develop novel classes of antibiotics, particularly ones against which it will be difficult to develop resistant bacterial strains.
Much of this work, however, is directed to synthesizing analogs of known drugs, such as cephalosporins and quinolones, that, while potentially useful for a short time, will inevitably also encounter bacterial drug resistance and become ineffective.
The use of oral antibacterials to treat otic infections in children has limited efficacy and creates a serious risk of pathogen resistance to the orally administered antibacterial agent.

Method used

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  • Ophthalmic And Otic Compositions Of Facially Amphiphilic Polymers And Oligomers And Uses Thereof

Examples

Experimental program
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Effect test

example 1

Antimicrobial Activity

Minimum Inhibitory Concentrations

[0832]The following three oligomers of the invention were screened for antimicrobial activity against a number of clinically relevant ocular pathogens.

[0833]Minimum Inhibitory Concentrations (MIC) of each of the 3 oligomers were determined using standard procedures for clinical ocular isolates of Ciprofloxacin Susceptible (CS) S. aureus (CSSA) (n=27), Ciprofloxacin Resistant (CR) S. aureus (CRSA) (n=28), CS S. epidermidis (CSSE) (n=26), CR S. epidermidis (CRSE) (n=26), St. pneumoniae (SP) (n=27), St. viridans group (SV), Moraxella Species (MS) (n=25), H. influenzae (HI) (n=26), P. aeruginosa (PA) (n=26), and Serratia marcescens (SM) (n=27).

[0834]The results are presented in Table 1. Data is expressed as MIC50, MIC90, in μg / ml for Oligomer 1, Oligomer 2, and Oligomer 3, respectively.

TABLE 1Oligomer 1Oligomer 2Oligomer 3MicrobialMIC50MIC90MIC50MIC90MIC50MIC90Strain(μg / ml)(μg / ml)(μg / ml)(μg / ml)(μg / ml)(μg / ml)CSSA0.1250.250.1250.250.5...

example 2

Ophthalmic Ointment Formulation

[0836]The following represents an example of a typical ophthalmic ointment formulation comprising an antimicrobial oligomer of the invention (oligomer 1 in Example 1 above).

Ophthalmic OintmentIngredientAmount (weight %)Oligomer 10.35Mineral Oil, USP2.0White petrolatum, USPq.s. 100

example 3

Ophthalmic Ointment Formulation

[0837]The following represents an example of a typical ophthalmic ointment formulation comprising an antimicrobial oligomer of the invention (oliogmer 2 in Example 1 above) and an anti-inflammatory agent.

Ophthalmic OintmentIngredientAmount (weight %)Oligomer 20.3Dexamethasone0.1Chlorobutanol, Anhydrous, NF0.5Mineral Oil, USP5.0White petrolatum, USPq.s. 100

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Abstract

The present invention discloses ophthalmic and otic compositions of facially amphiphilic antimicrobial polymers and oligomers and their uses, including their use in methods for treating and preventing ophthalmic infections and otic infections in humans and animals.

Description

CROSS-REFERENCE TO RELATED APPLICATIONS[0001]This application claims priority to U.S. provisional application Ser. No. 60 / 882,800 filed Dec. 29, 2006, which is incorporated herein by reference in its entirety.FIELD OF THE INVENTION[0002]The present invention relates to antimicrobial compositions of facially amphiphilic antimicrobial polymers and oligomers useful for the treatment or prevention of ophthalmic and otic infections. The present invention also relates to methods of using the compositions for treating and / or preventing ophthalmic and otic infections.BACKGROUND OF THE INVENTION[0003]Bacterial drug resistance is a significant current health problem throughout the world. Multiple drug resistance is being commonly seen in a number of human pathogens (see, e.g., Hiramatsu et al., J. Antimicrob. Chemother., 1998, 40, 311-313 and Montecalvo et al., Antimicro. Agents Chemother., 1994, 38, 1363-1367, and the incidence of drug-resistant hospital infections is growing at a rapid rate...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/74A61P27/02
CPCA61K9/0046A61K9/0048A61K9/0051A61K31/74A61K47/06A61K47/38A61K47/183A61K47/186A61K2300/00A61K31/506C07D239/02C07D239/24C07D239/28C07D403/14A61K31/573A61P23/00A61P27/02A61P27/06A61P27/16A61P29/00A61P31/00A61P31/02A61P31/04A61P31/10A61P31/12A61P31/22A61P37/08A61P43/00A61P9/12Y02A50/30A61K9/06A61K9/08
Inventor SCOTT, RICHARD W.
Owner POLYMEDIX
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