HTCC-HA Microgel Ointment for High Drug Loading
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Current microgel drug delivery systems face challenges such as the use of toxic chemical cross-linking agents, low drug loading leading to waste and increased costs, and inability to achieve long-term sustained release due to easy drug diffusion.
Innovation Solution
A method for preparing a sustained-release microgel ointment with high drug loading using a mixture of 2-hydroxypropyltrimethyl ammonium chloride chitosan (HTCC) and hyaluronic acid (HA) through electrostatic interaction, followed by drug addition, concentration, and thickening to enhance drug loading and sustained release.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Stability of the object's composition
If chemical cross-linking agents are used to prepare microgels, then the microgel structure is stable, but the preparation process becomes toxic and unsafe
Solution Approach 1:
The patent replaces chemical cross-linking with physical cross-linking mechanisms, specifically using electrostatic interactions between oppositely charged polymers (cationic chitosan and anionic alginate) to form stable microgel structures without toxic chemical agents. This substitution of chemical bonding with physical interactions resolves the contradiction between structural stability and toxicity.
Solution Approach 2:
The patent employs composite materials formed by combining cationic and anionic polymers that cross-link through electrostatic interactions. This composite approach creates stable microgel networks using natural, biocompatible materials, eliminating the need for synthetic chemical cross-linking agents while maintaining structural integrity.
2Ease of manufacture
If traditional immersion method is used for drug loading, then the process is simple, but the drug loading efficiency is low leading to waste of active ingredients
Solution Approach 1:
The patent changes the fundamental parameter of drug loading by incorporating drugs directly into the microgel structure during the formation process rather than subsequent immersion. This in-situ incorporation method ensures complete drug entrapment within the microgel network, eliminating waste from equilibrium concentration limitations while maintaining process simplicity.
Solution Approach 2:
The patent performs preliminary drug incorporation during microgel formation, adding the drug to the polymer solution before cross-linking occurs. This preliminary action ensures the drug is trapped within the developing microgel structure, achieving high loading efficiency without requiring complex post-processing steps.
3Device complexity
If physical diffusion drives drug release from microgel, then the release mechanism is simple, but the sustained release duration is limited due to rapid diffusion
Solution Approach 1:
The patent uses composite microgel structures with tightly cross-linked networks formed from cationic and anionic polymers. This composite structure creates a more dense and controlled matrix that slows drug diffusion while maintaining a relatively simple release mechanism, thereby extending sustained release duration without significantly increasing system complexity.
Solution Approach 2:
The patent changes the physical parameters of the microgel matrix by using double-crosslinked structures and controlling polymer concentration and molecular weight. These parameter changes reduce the mesh size and increase the density of the gel network, which slows drug diffusion rates and extends release duration while keeping the release mechanism relatively simple.
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 method achieves high drug loading and sustained release, reducing waste and preparation costs, while ensuring environmental friendliness and biological safety, with a release rate exceeding 90% in 48 hours.
Implementation Method 1
2-hydroxypropyltrimethyl ammonium chloride chitosan (HTCC) is a linear cationic polyelectrolyte, while hyaluronic acid (HA) is a linear anionic polyelectrolyte
Implementation Method 2
concentrating the mixture
Data Source
AI summary
Disclosed is a sustained-release microgel ointment with high drug loading and a preparation method and use thereof. HTCC aqueous solution and HA aqueous solution are mixed uniformly to obtain the microgel aqueous solution. A drug is mixed with the microgel aqueous solution and concentrated, and a thickening agent is added and mixed evenly to obtain the sustained-release microgel ointment with high drug loading. The HA and HTCC form a microgel through electrostatic action, which is safe and convenient. The concentration step increases the concentration of the drug solution outside the microgel, which can increase the drug loading of the microgel. Drugs not loaded in the microgel inhibited the drug from being released from the microgel, prolonging the sustained release time of the microgel. The thickener transforms the drug-loaded microgel suspension into a paste, facilitating to applying the drug on the skin surface. Meanwhile, the drug added can be used at 100%, reducing the cost of microgel ointment. The ointment can be used to prepare a medicine for treating histamine-independent pruritus and analgesia.