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Covalent Binding of BMP-2 on Surfaces Using a Self-assembled Monolayer Approach
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Covalently binding mucoadhesive polymers: N-hydroxysuccinimide grafted polyacrylates
Claudia Menzel1, Moritz Hauser1, Amelie Frey1
1Center for Chemistry and Biomedicine, Department of Pharmaceutical Technology, Institute of Pharmacy, University of Innsbruck, Innrain 80/82, 6020 Innsbruck, Austria.
Summary
Researchers developed novel mucus-binding polymers by attaching N-Hydroxysuccinimide (NHS) to polyacrylic acid (PAA). This PAA-NHS conjugate significantly enhances mucoadhesion, showing increased viscosity, adhesion time, and detachment force for potential pharmaceutical applications.
Area of Science:
- Polymer Chemistry
- Biomaterials Science
- Pharmaceutical Sciences
Background:
- Mucoadhesion is crucial for drug delivery systems to prolong residence time at mucosal surfaces.
- Developing effective mucoadhesive polymers requires strategies to enhance interactions with mucus glycoproteins.
- Targeting amino groups in mucus offers a specific approach for covalent mucoadhesion.
Purpose of the Study:
- To synthesize and characterize novel covalently mucus-binding polymers.
- To functionalize polyacrylic acid (PAA) with N-Hydroxysuccinimide (NHS) esters for targeting amino groups in mucus.
- To evaluate the mucoadhesive properties of the synthesized PAA-NHS conjugates.
Main Methods:
- Polyacrylic acid (PAA) was modified with N-Hydroxysuccinimide (NHS) using N,N'-dicyclohexylcarbodiimide (DCC) coupling.
- Chemical structure and coupling efficiency were confirmed using FTIR and UV spectroscopy.
- Mucoadhesion was assessed through rheological studies, tensile force measurements, and adhesion time evaluations on intestinal mucosa.
Main Results:
- Successful synthesis of PAA-NHS conjugates with high NHS coupling rates (876–1820 µmol/g).
- PAA-NHS demonstrated a 7.9-fold increase in mucus viscosity and a 5.5-fold longer adhesion time compared to unmodified PAA.
- Tensile force tests showed a 1.7-fold higher maximum detachment force and a 2.7-fold increase in total work of adhesion for PAA-NHS.
Conclusions:
- Coupling NHS to polymers is a viable strategy for creating potent mucoadhesive materials.
- PAA-NHS exhibits significantly enhanced mucoadhesive properties, indicating its potential as a novel excipient.
- These findings support the development of advanced drug delivery systems utilizing covalently binding mucoadhesive polymers.
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