Ionic Nanostructured Complex Antibacterial Agent for Drug-Resistant Infections

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Solution Overview

Problem

Current antimicrobial agents face challenges in effectively treating drug-resistant bacterial infections, particularly multidrug-resistant tuberculosis, due to increased resistance and the need for new compounds with tailored biocidal properties and mechanisms of action.

Innovation Solution

Development of an ionic nanostructured complex (INSC) composed of proteins, carbohydrates, and iodine, formed through a four-stage complexation reaction involving interaction of carbohydrates and proteins with metal salts, intercalation of iodine, introduction of terminal amino acids with electron-donating functional groups, and further iodine intercalation, to create a structured antimicrobial agent with enhanced immunotropic action.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional antibiotics are used to treat bacterial infections, then they can suppress activity of infectious agents, but increased drug resistance of pathogens reduces their effectiveness

Engineering Contradiction:
Improveeffectiveness of antimicrobial treatmentVSAvoiddrug resistance of pathogens
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent changes the chemical parameters of the antimicrobial agent by using iodine in a specific oxidation state (I2) rather than conventional antibiotics. The iodine forms a complex with carbohydrates and proteins at controlled concentrations (0.5-5.0 g/L iodine, 1-10 g/L carbohydrate, 0.1-5 g/L protein), creating a new chemical entity that bypasses antibiotic resistance mechanisms while maintaining bactericidal activity against drug-resistant strains including MRSA and multidrug-resistant tuberculosis

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates a composite antimicrobial system consisting of iodine complexed with carbohydrates and proteins. This composite structure (iodine-carbohydrate-protein complex) combines the bactericidal properties of iodine with the stabilizing and immunomodulatory effects of biopolymers, resulting in an agent that is effective against drug-resistant bacteria while reducing toxicity compared to free iodine

Inventive Principle:
Principle #40Composite materials

2Productivity

If iodine-based antimicrobial agents are used to achieve broad-spectrum activity, then they can penetrate cell membranes effectively, but toxicity increases

Engineering Contradiction:
Improvebactericidal activity and membrane penetrationVSAvoidtoxicity to host cells
Core Design Contradiction:
ProductivityVSObject-affected harmful factors

Solution Approach 1:

The patent controls the oxidation state of iodine (maintaining it as I2 rather than converting to more reactive forms like hypoiodous acid) and regulates the concentration of iodine within a specific range (0.5-5.0 g/L) combined with carbohydrates and proteins. This parameter control reduces toxicity while preserving the ability of iodine to penetrate bacterial cell membranes and interact with amino acid residues

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent uses carbohydrates and proteins as intermediaries that complex with iodine. These biopolymers act as carriers that deliver iodine to bacterial cells while protecting host tissues from direct exposure to high concentrations of free iodine, thereby reducing toxicity. The complex also enhances immunomodulatory effects through interaction with immunocompetent cells

Inventive Principle:
Principle #24Intermediary (Mediator)

Applied Scientific Principles

This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.

Function Achieved in This Case

The resulting antibacterial agent (ABA) demonstrates increased efficiency in vivo by activating immunocompetent cells, showing bactericidal activity against drug-resistant strains, including MRSA and Mycobacterium tuberculosis, while also exhibiting radioprotective and weak anti-tumor effects, and can be formulated into various pharmaceutical forms for enhanced therapeutic efficacy.

Implementation Method 1

molecular iodine can easily pass through bi-lipid cell membranes of microorganisms and penetrate into a cell

Methodology Applied
Scientific EffectMembrane penetration: Permeation

Implementation Method 2

ability of iodine (elemental iodine, hypoiodine acid, iodine cation) to interact with NH2-groups of amino acids (lysine, histidine, arginine, etc.), as well as nucleotides (adenine, cytosine, guanine) forming N-iodine derivatives

Methodology Applied
Scientific EffectChemical bonding: Chemical Bonding

Implementation Method 3

there is an oxidation of SH-groups of cysteine taking place, resulting in disruption of protein synthesis

Methodology Applied
Scientific EffectOxidation: Oxidation

Implementation Method 4

Interaction with phenolic groups of iodine tyrosine leads to breaking of hydrogen bonds in these amino acids

Methodology Applied
Scientific EffectHydrogen bond disruption:

Implementation Method 5

Affecting double carbon bonds of unsaturated fatty acids, iodine thereby changes the properties of lipids

Methodology Applied
Scientific EffectChemical addition: Chemical Bonding

Implementation Method 6

interaction of carbohydrates and proteins with metal salts, intercalation of iodine

Methodology Applied
Scientific EffectComplexation:

Implementation Method 7

intercalation of 5-95% of the required amount of iodine into a complex formed during the first stage of complexation reaction

Methodology Applied
Scientific EffectIntercalation:

Data Source

PatentUS10251939B2Antibacterial agent for treating infectious diseases of bacterial origin
Publication Date: 2019.04.09 SCI CENT OF ANTI INFECTIOUS DRUGS JOINT CO
  • US10251939B2 patent drawing
  • US10251939B2 patent drawing
  • US10251939B2 patent drawing

AI summary

The invention relates to medicine, namely to the antimicrobial agent for the treatment of infectious bacterial diseases including hospital infections and drug-resistant TB which represents the ion nanostructured complex (INSC) synthesized from carbohydrates proteins and/or polypeptides (albumins, interleukins, interferons, signaling proteins, etc), which are to enhance the antimicrobial activity in vivo, by activating immune cells that contain at least one terminal amino acid such as Phe, Ala, Val, Ala, Leu, Ile, and others with electron-donor functional groups, iodine and halides of the alkali and alkaline earth elements in the fourth stage at a certain ionic strength; an antibacterial agent increases: the susceptibility of bacteria, including antibiotic-resistant, to antibiotics; activity of monocytes and macrophages; efficiency of antibiotic treatment of hospital infections and drug-resistant TB; it also has antiviral activity, stimulates hematopoietic function of bone marrow; has an antitumor effect and radioprotective properties; in acceptable concentrations of components can be used as non-pharmaceutical agent (BAFS or parapharmaceutical); is presented in the pharmacological form suitable for parenteral, oral, external, or other application. INSC has the formula [{(Ln (MeI3)+) y [Me (Lm) I]+x} (Cl—) y+x+k] with M=30-300 kDa.