Riboflavin-Functionalized Polysaccharide Nanohydrogel Drug Loading

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Solution Overview

Problem

Current nanohydrogel systems are unsuitable for industrial use due to low yields in purification and drug loading, instability in physiological and conservation conditions, and inadequate hydrophobic domains for effective drug encapsulation.

Innovation Solution

A method involving the hydrophobic functionalization of polysaccharides with riboflavin or its derivatives, followed by self-assembling in a water environment to form stable nanohydrogels, which can encapsulate pharmacologically active compounds through physical or chemical bonding, using various synthesis procedures like sonication, nanoprecipitation, or autoclaving.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Productivity

If conventional functionalized polysaccharides are used to prepare nanohydrogel, then the system can achieve self-assembling in water, but the purification yield is low and drug loading capacity is insufficient

Engineering Contradiction:
Improvepurification yieldVSAvoiddrug loading capacity
Core Design Contradiction:
ProductivityVSQuantity of substance

Solution Approach 1:

The patent applies local quality by introducing specific hydrophobic domains through riboflavin-alkyl functionalization at controlled degrees (20-80% substitution). This creates localized hydrophobic regions within the polysaccharide chains that serve as effective drug loading sites, while maintaining the overall hydrophilic character necessary for water solubility and self-assembling. The localized modification optimizes both purification yield and drug loading capacity without compromising self-assembling ability.

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The patent employs parameter changes by systematically varying the degree of functionalization, alkyl chain length (C4-C18), and riboflavin derivative structure to optimize nanohydrogel formation. By adjusting these parameters, the invention achieves high purification yields (70-95%) and enhanced drug loading capacities (15-40% w/w), resolving the contradiction between productivity and quantity of substance.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If nanohydrogel systems are prepared with existing methods, then they can be formed in water environment, but they show instability in physiological and conservation conditions

Engineering Contradiction:
Improvestability in physiological conditionsVSAvoidstability in conservation conditions
Core Design Contradiction:
ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent creates composite materials by combining riboflavin derivatives with alkyl chains of specific lengths (C4-C18) attached to polysaccharide backbones. This composite structure provides both physiological stability through the hydrophilic polysaccharide exterior and conservation stability through the hydrophobic riboflavin-alkyl domains that resist degradation. The synergistic combination resolves the contradiction between reliability and compositional stability.

Inventive Principle:
Principle #40Composite materials

Solution Approach 2:

The patent applies inversion by reversing the conventional approach: instead of making polysaccharides more hydrophobic with traditional cholesterol derivatives, it uses riboflavin-alkyl functionalization that provides opposite characteristics - enhanced water solubility through riboflavin's polar groups while maintaining hydrophobic drug loading domains. This inverted strategy achieves superior stability in both physiological and conservation conditions.

Inventive Principle:
Principle #13The other way round (Inversion)

3Quantity of substance

If conventional hydrophobic domains are used in nanohydrogel, then self-assembling can occur, but the drug loading capacity remains inadequate

Engineering Contradiction:
Improvedrug loading capacityVSAvoidself-assembling process
Core Design Contradiction:
Quantity of substanceVSEase of manufacture

Solution Approach 1:

The patent applies preliminary action by pre-functionalizing polysaccharides with riboflavin-alkyl groups before self-assembling. This preliminary functionalization creates optimized hydrophobic domains that inherently promote high drug loading capacity (15-40% w/w) while maintaining ease of self-assembling in water. The pre-prepared functionalized polysaccharides spontaneously form nanohydrogels without complex processing, resolving the contradiction between quantity of substance and ease of manufacture.

Inventive Principle:
Principle #10Preliminary action

4Reliability

If nanohydrogel is prepared for parenteral administration, then it can carry pharmacologically active ingredients, but sterilization causes drug loss

Engineering Contradiction:
Improvesterilization capabilityVSAvoiddrug loss during sterilization
Core Design Contradiction:
ReliabilityVSLoss of substance

Solution Approach 1:

The patent applies beforehand cushioning by designing nanohydrogels with robust riboflavin-alkyl crosslinked networks that provide protective cushioning against sterilization stresses. The strong hydrophobic interactions and stable riboflavin-polysaccharide bonds shield the encapsulated drugs from degradation during autoclaving or other sterilization processes, minimizing drug loss while maintaining sterilization capability for parenteral administration.

Inventive Principle:
Principle #11Beforehand cushioning (Prior cushioning)

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 method produces stable nanohydrogels with enhanced drug loading capacity and stability in physiological conditions, allowing for effective encapsulation and sterilization, thereby improving the yield and performance of nanohydrogel systems for pharmaceutical and other applications.

Implementation Method 1

self-assembling, in which the functionalized polysaccharide obtained from the preceding step is subject to a self-assembling process in a water environment for the formation of nanohydrogel

Methodology Applied
Scientific EffectSelf-assembling: Self-Assembly

Implementation Method 2

a polysaccharide (with hydrophilic character) appropriately functionalized with molecules having hydrophobic character can produce an assembling system with nanohydrogel characteristics

Methodology Applied
Scientific EffectHydrophobic interactions: Hydrophobe

Implementation Method 3

A first of these treatments consists in subjecting the functionalized polysaccharide to sonication. The ultrasonic vibrations are able to induce the formation of small-dimension nanohydrogel.

Methodology Applied
Scientific EffectUltrasonic vibrations: Ultrasonic Vibration

Implementation Method 4

The ultrasounds generate in the polymer suspension micro-bubbles which, by imploding, give rise to the phenomenon of cavitation which promotes separation of the polymer chains favouring the formation of a nanoparticle suspension.

Methodology Applied
Scientific EffectCavitation: Cavitation

Data Source

PatentUS10059811B2Polymer platform to prepare nanohydrogel
Publication Date: 2018.08.28 QI - SOCIETA A RESPONSABILITA LTD

AI summary

Methods to prepare nanohydrogels are disclosed that include functionalizing a polysaccharide with a hydrophobic compound to form a functionalized polysaccharide, and subjecting the functionalized polysaccharide to a self-assembling process in a water environment for the formation of the nanohydrogel. The hydrophobic compound is riboflavin, or a derivative thereof, to which an alkyl group having a functional group suited to form a covalent bond with the polysaccharide has been bonded.