Modified Chitosan Nanoparticles for Vitamin D Bioavailability

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Solution Overview

Problem

Vitamin D supplements face challenges with impaired oral bioavailability, especially in individuals with biliary or hepatic dysfunction, and its active metabolites' generation is impaired in renal and hepatic disorders, due to susceptibility to oxidation and short half-life.

Innovation Solution

Development of nanoformulations using modified chitosan polymers covalently linked with fatty acids, amino acids, and other entities to encapsulate vitamin D derivatives and metabolites, providing protection against oxidation and enhancing bioavailability through nanoparticle delivery systems for both topical and oral administration.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If vitamin D is administered as traditional supplements, then it provides vitamin D intake, but oral bioavailability is impaired and absorption is reduced in individuals with biliary or hepatic dysfunction

Engineering Contradiction:
Improveoral bioavailabilityVSAvoidimpaired absorption in biliary or hepatic dysfunction
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent uses modified chitosan polymers as intermediary carriers to deliver vitamin D. The chitosan polymer with attached fatty acids acts as a mediator that facilitates vitamin D absorption through intestinal membranes, bypassing the impaired biliary or hepatic pathways. This intermediary system enables vitamin D delivery even when traditional absorption routes are compromised.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention changes the physical and chemical parameters of vitamin D by incorporating it into modified chitosan polymer structures. By attaching fatty acids to chitosan and complexing vitamin D with this modified polymer, the solubility, stability, and bioavailability parameters of vitamin D are improved, enabling effective absorption despite hepatic or biliary dysfunction.

Inventive Principle:
Principle #35Parameter changes

2Duration of action of stationary object

If vitamin D is stored traditionally, then it is available for supplementation, but it is susceptible to oxidation and has short half-life

Engineering Contradiction:
Improvehalf-lifeVSAvoidsusceptibility to oxidation
Core Design Contradiction:
Duration of action of stationary objectVSObject-affected harmful factors

Solution Approach 1:

The modified chitosan polymer creates a protective environment around vitamin D that shields it from oxidation. The polymer structure acts as a barrier, isolating vitamin D from oxidative agents in the biological environment, thereby extending its half-life and maintaining its stability during storage and circulation.

Inventive Principle:
Principle #39Inert atmosphere (Inert environment)

Solution Approach 2:

The invention creates a composite material system where vitamin D is complexed with modified chitosan polymer. This composite structure combines the stability and protective properties of the polymer with the biological activity of vitamin D, resulting in a formulation that resists oxidation and extends half-life compared to pure vitamin D.

Inventive Principle:
Principle #40Composite materials

3Reliability

If modified chitosan polymer is used to encapsulate vitamin D, then bioavailability is enhanced and protection against oxidation is provided, but the formulation complexity increases

Engineering Contradiction:
ImprovebioavailabilityVSAvoidformulation complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The complex formulation is broken down into modular components: chitosan polymer, fatty acid attachments, and vitamin D loading. This segmentation allows each component to be optimized independently and simplifies the overall manufacturing process while maintaining the benefits of the complex structure.

Inventive Principle:
Principle #1Segmentation

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 nanoformulations stabilize vitamin D, improve its bioavailability, and efficacy in treating conditions like osteoporosis, skin aging, and cardiovascular diseases by sustained release and enhanced absorption, overcoming the limitations of traditional vitamin D supplements.

Implementation Method 1

nanoparticles, each nanoparticle comprising a modified chitosan polymer encapsulating at least one vitamin D derivative

Methodology Applied
Scientific EffectEncapsulation:

Implementation Method 2

providing protection against oxidation and enhancing bioavailability through nanoparticle delivery systems

Methodology Applied
Scientific EffectOxidation protection: Oxidation

Implementation Method 3

enhancing bioavailability through nanoparticle delivery systems for both topical and oral administration

Methodology Applied
Scientific EffectNanoparticle delivery:

Implementation Method 4

improve its bioavailability, and efficacy in treating conditions like osteoporosis, skin aging, and cardiovascular diseases by sustained release and enhanced absorption

Methodology Applied
Scientific EffectSustained release:

Implementation Method 5

modified chitosan polymer comprises chitosan covalently linked to at least one entity selected from the group consisting of fatty acids (omega-3-fatty acids-EPA and/or DHA), amino acids

Methodology Applied
Scientific EffectCovalent bonding: Chemical Bonding

Data Source

PatentUS8968790B2Nanoformulation of vitamin D derivatives and/or vitamin D metabolites
Publication Date: 2015.03.03 MOUSA SHAKER A
  • US8968790B2 patent drawing
  • US8968790B2 patent drawing

AI summary

A nanoformulation that includes loaded nanoparticles. Each nanoparticle includes a modified chitosan polymer encapsulating at least one vitamin D derivative, at least one vitamin D metabolite, or combinations thereof. The modified chitosan polymer includes chitosan covalently linked to at least one entity selected from the group consisting of fatty acids (omega-3-fattay acids), amino acids, deoxycholic acid, alginate, arginine-alginate, hyaluronic acid, collagen, collagen-hydroxyapatite, poly(lactic-co-glycolic acid) (PLGA), and combinations thereof. A structure includes a medium and the nanoformulation, wherein the nanoparticles are dispersed in the medium. A method of using the nanoformulation to treat a disorder and improve efficacy of current therapies where resistance develop in a patient includes administering to the patient a therapeutically effective amount of the nanoformulation for treating the disorder. A nano-cosmetic formulation, comprising a cosmetic includes the nanoformulation, wherein the modified chitosan polymer encapsulates the at least one vitamin D derivative, and wherein the at least one vitamin D derivative encompasses 0.1 to 20.0 wt % of the nano-cosmetic formulation's total weight.