A pH dependent delivery of mesalazine from polymer coated and drug-loaded SBA-16 systems

Area of Science:

• Materials Science
• Nanotechnology
• Pharmaceutical Sciences

Background:

• Mesalazine (5-aminosalicylic acid) is a poorly soluble drug used for inflammatory bowel disease.
• Developing effective oral delivery systems for mesalazine is crucial for improving therapeutic outcomes.
• Mesoporous silica nanoparticles offer potential as drug carriers due to their high surface area and tunable pore sizes.

Purpose of the Study:

• To synthesize and functionalize SBA-16 silica nanoparticles with amino groups.
• To load mesalazine into the functionalized SBA-16 carrier using wet milling.
• To evaluate polymer coating strategies for controlled mesalazine release and assess cytotoxicity.

Main Methods:

• SBA-16 silica synthesis and post-synthesis amination.
• Mesalazine loading via wet milling at various drug/carrier ratios.
• Characterization using XRD, TEM, N2 physisorption, thermal analysis, FT-IR, and solid-state NMR.
• Drug-loaded systems coated with Eudragit S or Eudragit S/RL.
• In vitro drug release studies and cytotoxicity assays.

Main Results:

• Successful synthesis and amination of SBA-16 silica.
• Efficient loading of mesalazine into the mesoporous carrier.
• Polymer coating significantly altered mesalazine release kinetics.
• Double coating with Eudragit S and Eudragit RL achieved sustained release in simulated intestinal conditions, preventing gastric burst release.
• Loading mesalazine into SBA-16 reduced its cytotoxicity towards epithelial cells.

Conclusions:

• Functionalized, polymer-coated SBA-16 mesoporous silica is a promising system for oral mesalazine delivery.
• The developed system offers sustained drug release in the intestine, enhancing therapeutic potential.
• This approach can mitigate mesalazine's cytotoxicity, improving its safety profile.