Peptide-Ionic Liquid Conjugates for Drug-Resistant Skin Infections
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Solution Overview
Problem
Current treatments for skin disorders, particularly complicated skin and soft tissue infections (cSSTI), are inadequate against multidrug-resistant bacteria and fungi, and there is a need for new options that can promote wound healing and address polymicrobial infections effectively.
Innovation Solution
Development of peptide-ionic liquid (PIL) conjugates, specifically combining cosmeceutical peptides with up to 10 amino acids and ionic liquids, which are covalently attached to the peptide's N-terminus or side chains, exhibiting antibacterial, antifungal, and collagenesis-inducing activities.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional antibiotics are used to treat skin infections, then treatment of susceptible bacteria is effective, but treatment fails against multidrug-resistant bacteria and fungi
Solution Approach 1:
The patent combines cosmeceutical peptides with ionic liquids to create a composite conjugate structure. This composite approach integrates the collagenesis-inducing capability of peptides with the broad-spectrum antimicrobial and permeation-enhancing properties of ionic liquids, achieving simultaneous activity against multidrug-resistant bacteria and fungi while promoting wound healing
Solution Approach 2:
The PIL conjugate is designed to perform multiple functions: it exhibits antibacterial activity against Gram-positive and Gram-negative bacteria, antifungal activity against Candida and Cladosporidium species, dermal permeation enhancement, and collagenesis induction. This multi-functional design allows a single agent to address polymicrobial infections and promote healing
2Reliability
If peptide-based antimicrobials are used, then activity against Gram-positive bacteria is achieved, but activity against Gram-negative bacteria and fungi is insufficient
Solution Approach 1:
By conjugating peptides with ionic liquids, the patent creates a composite that combines the properties of both components. The ionic liquid moiety provides broad-spectrum antimicrobial activity including against Gram-negative bacteria and fungi, while the peptide component maintains its collagenesis-inducing capability
Solution Approach 2:
The patent modifies the chemical structure by attaching ionic liquid moieties to peptides, changing the physical and chemical parameters of the original peptide. This structural modification enables the conjugate to interact with and disrupt membranes of Gram-negative bacteria and fungi while retaining biological activity
3Ease of operation
If ionic liquids are used as dermal permeation enhancers, then topical delivery is improved, but intrinsic antimicrobial activity may be insufficient for severe infections
Solution Approach 1:
The patent merges the dermal permeation-enhancing property of ionic liquids with the antimicrobial and collagenesis-inducing properties of peptides into a single conjugate molecule. This merging allows the PIL to simultaneously enhance its own topical delivery and provide potent antimicrobial activity
Solution Approach 2:
The conjugate structure combines the permeation-enhancing ionic liquid component with the bioactive peptide component, creating a composite that exhibits both enhanced dermal penetration and intrinsic antimicrobial potency, eliminating the need for separate delivery and therapeutic agents
Data Source
AI summary
A peptide-ionic liquid conjugate for the prevention and/or treatment of skin disorders. The peptide-ionic liquid conjugate comprises a cosmeceutical peptide comprising up to 10 amino acids and at least one ionic liquid comprising saturated or unsaturated hydrocarbon chain substituents from C1 to C18. The peptide-ionic liquid conjugates herein disclosed are suitable against skin disorders, such as, e.g., melanoma, non-melanoma skin cancers, diabetic foot ulcers, venous leg ulcers, pressure ulcers, acne, candidiasis, cellulitis, dermatophytoses, erysipelas, folliculitis, impetigo, psoriasis, rosacea, or eczema (atopic dermatitis), since they present potent activity against either antibiotic-susceptible strains or multidrug resistant clinical isolates of both Gram-positive and Gram-negative, a bactericidal type of action, anti-inflammatory and immunomodulatory effects, and collagenesis-inducing effects. Further disclosing a topical composition comprising the peptide-ionic liquid conjugates and uses thereof.