Polysaccharide Matrix for Controlled Drug Release
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Solution Overview
Problem
Current treatments for osteoarthritis, particularly those involving aqueous parenteral formulations, face challenges with poor water solubility of active ingredients and inadequate control over drug release, leading to issues like precipitation, side effects, and reduced efficacy.
Innovation Solution
A novel composition featuring a cyclodextrin and active ingredient clathrate homogeneously dispersed in a polysaccharide polymer matrix, specifically hyaluronic acid and a chitosan derivative with lactose, which stabilizes and controls the release of the active ingredient, providing a viscosupplementation effect alongside pharmacological action.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If active ingredients are administered in aqueous parenteral formulations, then pharmacological effect is achieved, but water solubility of active ingredients is poor leading to precipitation and reduced efficacy
Solution Approach 1:
The patent employs cyclodextrins as intermediary molecules that form inclusion complexes with hydrophobic active ingredients. The cyclodextrin's hydrophilic exterior and hydrophobic interior cavity allow it to solubilize poorly water-soluble drugs, thereby improving their stability and efficacy in aqueous formulations without requiring cross-linked polymer matrices.
2Duration of action of moving object
If cross-linked polymer matrices are used to control drug release, then release control is improved, but side effects increase and safety profile worsens
Solution Approach 1:
The patent extracts and eliminates the cross-linking step from the formulation process. Instead of using cross-linked polymer matrices that cause adverse reactions, the invention relies on cyclodextrin inclusion complexes and physical entrapment within linear polysaccharide matrices to achieve controlled drug release, thereby maintaining duration of action while improving safety.
3Reliability
If NSAIDs are administered for analgesic effect, then pain relief is achieved, but gastrointestinal complications and cardiovascular risk increase
Solution Approach 1:
The patent changes the formulation parameters by using cyclodextrin-based inclusion complexes that modify the release profile and local concentration of analgesic agents. This approach maintains effective pain relief while reducing the systemic exposure and local irritation that cause gastrointestinal complications and cardiovascular risks associated with conventional NSAID formulations.
4Reliability
If steroids are administered for anti-inflammatory effect, then short-term pain relief is achieved, but inflammation and cartilage atrophy occur
Solution Approach 1:
The patent introduces dynamic control of drug release through cyclodextrin inclusion complexes and polysaccharide matrix interactions. This allows for sustained, controlled release of anti-inflammatory agents, extending the duration of therapeutic effect beyond the short-term relief provided by conventional steroid injections, while maintaining lower peak concentrations to reduce cartilage atrophy and inflammatory side effects.
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 composition ensures complete or partial solubilization of the active ingredient in an aqueous environment, stabilizes its physical form, and modulates its release, enhancing therapeutic efficacy while minimizing side effects and improving treatment outcomes for musculoskeletal diseases.
Implementation Method 1
compositions comprising a clathrate consisting in a cyclodextrin and an active ingredient
Implementation Method 2
modulates its release
Implementation Method 3
aqueous solution of a polysaccharide polymer matrix
Implementation Method 4
providing a viscosupplementation effect alongside pharmacological action
Data Source
Figure 1
AI summary
The present application describes compositions that can be used for the controlled release of pharmacological active ingredients from a viscoelastic aqueous polysaccharide matrix, and their potential use in the treatment of different stages of musculoskeletal diseases. The combination of drug release modulation and the viscoelastic nature of the composition makes possible the use thereof in the treatment of acute and chronic phases of musculoskeletal diseases characterized by an inflammatory state, and where a therapeutic effect and a viscosupplemental contribution are required.