Silicone Elastomer Octenidine Release via Cyclodextrin Complexation
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Solution Overview
Problem
Existing silicone elastomer compositions for dermal patches face challenges with catalyst poisoning, particularly with platinum catalysts, due to the presence of active substances containing nitrogen, sulfur, or phosphorus, leading to inefficient polymerization and poor delivery kinetics of hydrophobic antiseptics like octenidine, resulting in burst delivery and rapid depletion.
Innovation Solution
Incorporating β-cyclodextrin into the silicone elastomer compositions forms a complex with octenidine, protecting the platinum catalyst from poisoning and stabilizing the emulsion, allowing for zero-order or near-zero-order release of octenidine over a prolonged period by forming a molecular 1:1 complex with octenidine dihydrochloride, which is solubilized in glycerol, thereby maintaining effective antiseptic concentrations at the wound site.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Productivity
If platinum catalyst is used for polymerization of silicone pre-elastomer, then polymerization efficiency is improved, but catalyst poisoning occurs due to nitrogen-containing active substances like octenidine
Solution Approach 1:
β-cyclodextrin acts as an intermediary substance that selectively binds to octenidine through host-guest complexation, forming a protective complex that prevents direct contact between the nitrogen-containing antiseptic and the platinum catalyst. This mediator approach allows the catalyst to function efficiently while the active substance remains available for controlled release.
Solution Approach 2:
The β-cyclodextrin is pre-mixed with octenidine to form a complex before the polymerization process begins. This preliminary complexation protects the catalyst from poisoning before it can occur, ensuring stable polymerization while maintaining the integrity of the active substance for subsequent controlled release.
2Quantity of substance
If hydrophobic antiseptic like octenidine is incorporated into silicone elastomer, then antiseptic delivery is achieved, but burst delivery and rapid depletion occur due to poor release kinetics
Solution Approach 1:
β-cyclodextrin serves as a mediator that forms a soluble complex with hydrophobic octenidine, enhancing its solubility in the glycerol phase and enabling controlled diffusion. This complexation prevents burst release by regulating the release kinetics through the cyclodextrin-octenidine interaction.
Solution Approach 2:
The solubility and release kinetics of octenidine are modified by forming a complex with β-cyclodextrin. This parameter change transforms the release profile from burst-type to sustained zero-order kinetics, extending the duration of antiseptic action while maintaining effective concentrations.
3Quantity of substance
If octenidine is solubilized in glycerol phase, then active substance release is enabled, but catalyst poisoning occurs due to nitrogen content in octenidine
Solution Approach 1:
β-cyclodextrin acts as a protective intermediary that binds to octenidine in the glycerol phase, preventing direct interaction between the nitrogen-containing antiseptic and the platinum catalyst during polymerization. The cyclodextrin cavity shields the catalyst from poisoning while allowing the complex to remain solubilized in the glycerol phase for subsequent release.
Data Source
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AI summary
Herein is disclosed an emulsion comprising a silicone pre-elastomer, glycerol, a cyclodextrin, and a metal catalyst suitable for use in the polymerization of the silicone pre-elastomer, a silicone elastomer formed from the emulsion and dermal patches for release of octenidine formed from the silicone elastomer. Further there is dis-closed methods of forming the emulsion, the silicone elastomer and the dermal patch.