Parallelepiped Alginate Delivery System for Controlled Release

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Solution Overview

Problem

Existing systems for the controlled delivery of biologically active substances, particularly those using alginate polymer matrices, face challenges in achieving reproducible and predictable kinetics, leading to poor absorption efficiency and increased risk of side effects due to uniform barriers and complex swelling and erosion processes.

Innovation Solution

A process for forming a three-dimensional structure with a parallelepiped shape using acid-hydrolyzed alginates and cellulose-based bridges, allowing for adjustable size and pH-dependent or cell-mediated release, enhancing bioavailability and absorption efficiency without increasing dosage.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of manufacture

If a uniform thickness barrier is used to enclose the biologically active substance, then the structure is simple to manufacture, but the delivery kinetics become unpredictable and absorption efficiency decreases

Engineering Contradiction:
Improveease of manufactureVSAvoiddelivery kinetics precision
Core Design Contradiction:
Ease of manufactureVSManufacturing precision

Solution Approach 1:

The patent applies local quality by creating a non-uniform barrier thickness where different regions have different thicknesses. This allows the barrier to provide protection in thicker regions while enabling controlled release in thinner regions, achieving both manufacturability and predictable delivery kinetics through spatial variation in barrier properties.

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The patent introduces dimensional variation by transitioning from a uniform one-dimensional thickness parameter to a three-dimensional non-uniform thickness distribution. This dimensional change allows the barrier to simultaneously provide protection and controlled release pathways, resolving the contradiction between simple manufacture and predictable kinetics.

Inventive Principle:
Principle #17Another dimension (Dimensionality change)

2Reliability

If the dosage of biologically active substance is increased to compensate for poor absorption efficiency, then the delivery system can achieve therapeutic effect, but side effects and intolerance increase

Engineering Contradiction:
Improvetherapeutic effect reliabilityVSAvoidside effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent changes the physical parameter of barrier thickness distribution to improve absorption efficiency. By optimizing the thickness parameter spatially, the system enhances bioavailability of the same dosage, thereby achieving therapeutic effects at lower doses and reducing side effects associated with higher dosages.

Inventive Principle:
Principle #35Parameter changes

3Reliability

If alginates are used to form a barrier for controlled delivery, then the biologically active substance can be protected during passage through the stomach, but the swelling and dissolution process becomes too complex to achieve reproducible kinetics

Engineering Contradiction:
Improveprotection reliabilityVSAvoidswelling process complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent applies preliminary action by pre-forming the non-uniform barrier structure before exposure to physiological conditions. The barrier is manufactured with predetermined thickness variations that control the release kinetics in advance, eliminating the need to rely on complex swelling and dissolution processes for kinetic control.

Inventive Principle:
Principle #10Preliminary action

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 process improves the absorption efficiency of biologically active substances by providing controlled release based on environmental conditions, reducing side effects, and enhancing pharmacokinetics and pharmacodynamics, while allowing for adaptable structure sizes and shapes for various substances.

Implementation Method 1

a) subjecting alginates to a process of acid hydrolysis

Methodology Applied
Scientific EffectAcid hydrolysis: Hydrolysis

Implementation Method 2

Hydration of alginic acid and alginate causes swelling thereof and formation of a high-viscosity gel

Methodology Applied
Scientific EffectSwelling:

Implementation Method 3

The delivery of the biologically active substance is indeed modulated by the diffusion of said substance through swelling of the polymer matrix

Methodology Applied
Scientific EffectDiffusion: Diffusion

Data Source

PatentEP3253416B1Process for obtaining a system for the controlled delivery of a biologically active substance and controlled delivery system obtained thereby
Publication Date: 2023.05.03 SUNTEKNA SAGL
  • EP3253416B1 patent drawingFigure 1
  • EP3253416B1 patent drawingFigure 2a~2b
  • EP3253416B1 patent drawingFigure 3a~3d

AI summary

The present invention relates to a process for obtaining a system for the controlled delivery of a biologically active substance allowing to obtain an effective delivery in terms of percentage of said biologically active substance that is absorbed by the organism. More particularly, the present invention relates to a process consisting in obtaining a controlled delivery system in which the biologically active substance is enclosed in a structure having a substantially parallelepiped shape with the desired shape and size, which can internally adapt to the biologically active substance to be carried and externally to the interaction with target cells (for example, enterocytes), thus optimizing the delivery modes of said biologically active substance. Advantageously, the process according to the invention allows to create parallelepiped structures with nanometric, micrometric or larger sizes, thereby making the controlled delivery system thus obtained suitable for a large variety of biologically active substances, including ions, molecules and macromolecules.