Antimicrobial compositions and methods

Abstract

Antimicrobial compositions, especially those useful when applied topically, particularly to mucosal tissues (i.e., mucous membranes), including a fatty acid ester, fatty ether, or alkoxide derivative thereof. The compositions can also include an enhancer component, a surfactant, a hydrophobic component, and / or a hydrophilic component. Such compositions provide effective topical antimicrobial activity and are accordingly useful in the treatment and / or prevention of conditions that are caused, or aggravated by, microorganisms (including viruses).

Description

BACKGROUND The use of antimicrobial agents plays an important part in current medical therapy. This is particularly true in the fields of dermatology as well as skin and wound antisepsis, where the most effective course of treatment for skin or mucous membranes (e.g., as in the nasal cavities and in particular the anterior nares), which are afflicted with bacterial, fungal, or viral infections or lesions, frequently includes the use of a topical antimicrobial agent. For decades medicine has relied primarily upon antibiotics to fight systemic as well as topical infections. For example, bacitracin, neomycin sulfate, polymyxin B sulfate, gentamicin, framycetin-gramicidin, lysostaphin, methicillin, rifampin, tobramycin, nystatin, mupirocin, and combinations thereof, as well as many others, have been used with varying success. Antibiotics are generally effective at very low levels and are often safe with very few, if any, side effects. Often antibiotics have little or no toxicity to ma...

AI Technical Summary

Benefits of technology

Compositions of the present invention provide effective topical antimicrobial activity and are accordingly useful in the local treatment and / or prevention of conditions that are caused, or aggravated by, microorganisms (including viruses, bacteria, fungi, mycoplasma, and protozoa) on skin and / or mucous membranes.

The compositions of the present invention can also be used for providing residual antimicrobial efficacy on a surface that results from leaving a residue or imparting a condition to the surface (e.g., skin, mucosal tissue, wound, or medical device that comes in contact with such tissues, but particularly skin, mucosal tissue, and / or wound) that remains effective and provides significant antimicrobial activity.

“Enhancer” means a component that enhances the effectiveness of the antimicrobial lipid component such that when the composition less the antimicrobial lipid component and the composition less the enhancer component are used separately, they do not provide the same level of antimicrobial activity as the composition as a whole. For example, an enhancer component in the absence of the antimicrobial lipid component may not provide any appreciable antimicrobial activity. The enhancing effect can be with respect to the level of kill, the speed of kill, and / or the spectrum of microorganisms killed, and may not be seen for all microorganisms. In fact, an enhanced level of kill is most often seen in Gram negative bacteria such as Escherichia coli. An enhancer may be a synergist such that when combined with the remainder of the composition, the composition as a whole displays an activity that is greater than the sum of the activity of the composition less the enhancer component and the composition less the antimicrobial lipid component.

Problems solved by technology

Thus, they may not retard, and can even enhance, wound healing.

Even though presurgical decolonization of the anterior nares using mupirocin has been shown to decrease the risk of surgical site infection by as much as 2 to 10 times (T. Perl et al., Ann. Pharmacother., 32:S7-S 16 (1998)), the high resistance rates to this antibiotic make it unsuitable for routine use.

Not only does resistance eliminate the ability of a medication to treat an affliction, but it can also put the patient at further risk, especially if the antibiotic is one that is routinely used systemically.

This nonspecific activity makes it difficult for resistance to develop to antiseptics.

These compounds, however, need to be used at concentrations that often result in irritation or tissue damage, especially if applied repeatedly.

Furthermore, unlike antibiotics, many antiseptics are not active in the presence of high levels of organic compounds.

Plus, they possess an even wider variety of side effects.

Additionally, due to the irritating nature many of these agents would be unsuitable for application to irritated or infected dermal tissue such as lesions from impetigo and shingles or sensitive tissues such as the nasal cavities and especially the anterior nares.

Also, many conventional antimicrobial compositions are too low in viscosity and / or too hydrophilic in nature to maintain sufficient substantivity and persistence to provide sufficient antimicrobial activity on moist tissue, such as the anterior nares or open, exuding, or infected lesions, and the like.

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