Phospholipid Gel Aptamer Delivery Sustained Release
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Solution Overview
Problem
There is a need for improved pharmaceutical compositions that can sustainably or controllably release aptamers, which are oligonucleotides used as therapeutic agents, to maintain effective concentrations in the body over extended periods, as existing formulations face challenges in achieving sufficient concentrations for clinical use and ensuring stability and distribution to target tissues.
Innovation Solution
The development of pharmaceutical compositions in the form of a gel, comprising a phospholipid or sphingomyelin, organic solvents such as propylene glycol or glycerol formal, and an aptamer, which form a gel structure to provide sustained or controlled release of the aptamer, enhancing its stability and tissue distribution.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If conventional immediate release formulations are used, then the drug can be administered frequently to maintain therapeutic levels, but the blood level fluctuations increase and side effects become more severe
Solution Approach 1:
The patent changes the physical state of the formulation from immediate-release to controlled-release by using gel matrices and encapsulation technologies. This transforms the release kinetics of the aptamer, maintaining steady blood levels and reducing fluctuations, thereby decreasing side effects while extending the duration of therapeutic effect.
Solution Approach 2:
The invention employs composite gel formulations combining hydrophilic and hydrophobic polymers, along with encapsulation materials, to create a matrix that controls aptamer release. This composite structure enables sustained release over extended periods, maintaining therapeutic levels without the peaks and troughs associated with immediate-release formulations.
2Quantity of substance
If aptamers are administered to achieve sufficient therapeutic concentrations, then the therapeutic efficacy improves, but the stability and distribution to target tissues become challenging
Solution Approach 1:
The patent introduces gel matrices and encapsulation materials as intermediaries between the aptamer and the biological environment. These carriers protect the aptamer from degradation, enhance its stability in circulation, and facilitate targeted delivery to specific tissues, thereby improving both stability and tissue distribution at therapeutic concentrations.
Solution Approach 2:
The invention uses flexible gel matrices and film-based encapsulation structures that can adapt to different tissue environments. These flexible carriers maintain aptamer stability while enabling penetration and distribution to target tissues, solving the challenge of delivering sufficient concentrations to specific anatomical locations.
3Ease of operation
If controlled- or sustained-release formulations are used, then the dosing frequency is reduced for enhanced convenience, but the formulation complexity increases
Solution Approach 1:
The patent develops universal gel formulations and encapsulation systems that can deliver multiple different aptamers using the same delivery platform. This multi-functional approach simplifies the overall complexity by providing a standardized controlled-release system that can be applied across different therapeutic indications, reducing dosing frequency while maintaining manageable formulation complexity.
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 gel-based compositions effectively maintain therapeutic levels of aptamers, improving their stability and distribution to target tissues, thereby enhancing their therapeutic efficacy and reducing dosing frequency.
Implementation Method 1
comprising a phospholipid or sphingomyelin, organic solvents such as propylene glycol or glycerol formal, and an aptamer, which form a gel structure to provide sustained or controlled release of the aptamer
Implementation Method 2
the phospholipid or sphingomyelin and at least one organic solvent are present in amounts sufficient to form a gel
Data Source
AI summary
The present invention relates to pharmaceutical compositions in the form of a gel for controlled- or sustained-release of an aptamer and to methods for treating or preventing a condition in an animal by administering to an animal in need thereof the pharmaceutical compositions.