Pharmaceutical Biodissolvable Gels Using Reverse Thermal Gelation
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Solution Overview
Problem
Existing drug delivery systems face challenges in maintaining bioavailability at the intended site of action over time, leading to suboptimal drug efficacy and increased dosing frequency due to degradation and rapid clearance, resulting in undesirable adverse effects.
Innovation Solution
A pharmaceutical composition comprising a reverse-thermal-gelation material that transitions from liquid to gel near body temperature, utilizing methylcellulose and gelation modulators like citrate and phosphate to achieve controlled drug release and prolonged exposure, allowing for reduced dosing frequency and improved patient compliance.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If conventional drug delivery systems are used, then drugs can be administered, but bioavailability is lost due to degradation and rapid clearance, requiring frequent dosing
Solution Approach 1:
The patent utilizes reverse thermal gelation, a phase transition phenomenon where the gel formulation transitions from liquid to gel state upon contact with body temperature. This phase change enables the formulation to remain injectable (liquid) during administration but form a sustained-release depot (gel) at the injection site, thereby extending drug action duration while maintaining reliable bioavailability through controlled release
Solution Approach 2:
The gel formulation is prepared in advance with specific gelation properties that will activate upon contact with body temperature. The preliminary formulation design ensures that when injected, it automatically undergoes phase transition to form a sustained-release depot, eliminating the need for frequent re-dosing while maintaining consistent drug levels
2Reliability
If drug dosing frequency is increased to maintain therapeutic levels, then bioavailability is improved, but adverse effects increase and patient compliance decreases
Solution Approach 1:
The reverse thermal gelation formulation provides periodic drug release through controlled diffusion from the gel depot, maintaining therapeutic levels over extended periods (weeks to months) without requiring frequent dosing. This periodic release pattern sustains bioavailability while minimizing peak-trough fluctuations that cause adverse effects
Solution Approach 2:
The phase transition from liquid to gel upon injection creates a depot that controls drug release kinetics, providing sustained therapeutic levels without the need for frequent dosing, thereby reducing adverse effects associated with high-frequency administration
3Duration of action of moving object
If gel formulations are used to prolong drug release, then dosing frequency is reduced, but injectability may be compromised due to increased viscosity
Solution Approach 1:
The formulation dynamically changes its physical state from liquid to gel upon contact with body temperature. During injection (at lower temperature), the formulation remains liquid and easily injectable. After injection, the temperature-induced phase transition transforms it into a gel depot that provides sustained drug release, thus resolving the contradiction between injectability and prolonged release duration
Solution Approach 2:
The reverse thermal gelation exploits the phase transition phenomenon where the formulation is liquid at room temperature (easy to inject) and transitions to gel state at body temperature (provides sustained release). This temperature-dependent phase change enables both easy administration and prolonged drug delivery without compromising either property
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 provides sustained drug delivery with reduced dosing frequency, achieving therapeutic effects for at least 5 days to 12 months by forming a semi-solid at body temperature, enhancing local drug exposure and minimizing systemic side effects.
Implementation Method 1
a reverse-thermal-gelation material that transitions from liquid to gel near body temperature
Data Source
AI summary
This disclosure relates to a pharmaceutical bio-dissolvable/bioerodible aqueous gel system optionally comprising an active pharmaceutical ingredient, wherein the pharmaceutical composition makes a transition from liquid to gel near the body temperature of a mammal These compositions may include a reversibly-gelling material, such as methylcellulose and a rheology modifier such as citrate.