Pure Melphalan Hydrogel via Self-Assembly
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Solution Overview
Problem
Current hydrogel preparations for small molecule melphalan drugs contain a large amount of carrier materials, leading to toxic side effects on normal tissues and low drug loading rates, making them unsuitable for in situ injection.
Innovation Solution
A 100% drug melphalan hydrogel is developed using melphalan or melphalan hydrochloride as raw materials, formed in a hydrophilic solvent at room temperature or physiological conditions, eliminating the need for carrier materials and allowing for in situ injection.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If conventional drug hydrogels are used to deliver melphalan, then the drug can be delivered to the lesion site, but the hydrogels contain a large amount of carrier materials (chitosan, poloxamer, polyethylene glycol) resulting in low drug loading rate and toxic side effects on normal tissues
Solution Approach 1:
The patent extracts and removes the carrier materials (chitosan, poloxamer, polyethylene glycol) from the hydrogel system, retaining only the active drug melphalan. This is achieved by designing a self-assembling melphalan-based hydrogel where the drug molecules themselves form the gel network through non-covalent interactions, eliminating the need for separate carrier materials and thereby achieving 100% drug loading while removing sources of toxicity to normal tissues
Solution Approach 2:
The patent changes the physical and chemical parameters of melphalan by controlling pH, temperature, and concentration conditions to induce self-assembly and gel formation. By adjusting these parameters, melphalan transitions from a soluble monomeric state to a self-assembled gel state, enabling the formation of a pure drug hydrogel without carrier materials and achieving high drug loading rate while reducing toxic side effects
2Duration of action of moving object
If conventional drug hydrogels are used, then the drug can be sustained in the lesion site, but the preparation process requires a large amount of carrier materials resulting in complex formulation and low drug loading rate
Solution Approach 1:
The patent removes carrier materials from the formulation, simplifying the preparation process to only require melphalan and physiological saline. This extraction of unnecessary components reduces formulation complexity while maintaining the sustained release capability through the self-assembled gel structure formed by melphalan molecules themselves
Solution Approach 2:
The melphalan molecules self-assemble into a gel network through non-covalent interactions (hydrogen bonding, π-π stacking, hydrophobic interactions) without requiring external carrier materials or complex crosslinking agents. The drug serves its own structural function, forming the gel matrix that enables sustained release while simplifying the overall preparation process
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 solution provides a pure melphalan hydrogel with a high drug loading rate, reducing toxic side effects and prolonging the duration of action on tumors, while simplifying the preparation method and avoiding the use of carriers.
Implementation Method 1
the small molecule melphalan hydrogel is formed at room temperature or physiological condition by means of making the melphalan drug in a hydrophilic solvent
Implementation Method 2
the hydrophilic solvent is used to form a hydrophilic environment to make melphalan form a gel state
Data Source
AI summary
The present disclosure relates to the field of hydrogel technology, and specifically relates to a small molecule melphalan hydrogel and a preparation method thereof. The small molecule melphalan hydrogel is made of melphalan drug or melphalan hydrochloride as raw materials, and it is formed at room temperature or physiological condition by means of making the melphalan drug in a hydrophilic solvent. The hydrophilic solvent includes any one of physiological saline, pure water, and phosphate buffered saline solution. The small molecule melphalan hydrogel provided by the present disclosure is an injectable hydrogel of 100% pure melphalan drug, the gel only contains small molecule melphalan drug, which solves the problems of containing a large amount of carrier materials and having a low drug loading rate in the field of hydrogel.