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Transport Properties of Ibuprofen Encapsulated in Cyclodextrin Nanosponge Hydrogels: A Proton HR-MAS NMR Spectroscopy Study
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New Ibuprofen Cystamine Salts With Improved Solubility and Anti-Inflammatory Effect
Simay Denizkusu1, Ece Sabuncu2, Hande Sipahi2
1Department of Chemistry, Bogazici University, 34342, Bebek, Istanbul, Turkey.
Chemistryopen
|October 14, 2024
Summary
Two new ibuprofen cystamine salts (IBU-CYS 1 and IBU-CYS 2) significantly enhance ibuprofen
Area of Science:
- Pharmaceutical Chemistry
- Drug Delivery Systems
- Medicinal Chemistry
Background:
- Ibuprofen, a widely used non-steroidal anti-inflammatory drug (NSAID), suffers from poor aqueous solubility, limiting its bioavailability and formulation options.
- Developing novel salt forms is a common strategy to improve the physicochemical properties and therapeutic efficacy of existing drugs.
- Cystamine, a diamine, has been explored for its potential therapeutic applications and as a counterion for salt formation.
Purpose of the Study:
- To synthesize and characterize novel ibuprofen cystamine salts (IBU-CYS 1 and IBU-CYS 2) to enhance ibuprofen's solubility and bioavailability.
- To evaluate the anti-inflammatory potential and cytotoxicity of the synthesized salts.
- To explore the feasibility of incorporating IBU-CYS2 into hydrogel formulations for enhanced drug delivery.
Main Methods:
- Synthesis of ibuprofen cystamine salts in 1:1 and 2:1 ratios.
- Characterization using spectroscopic (NMR, FT-IR, UV-Vis), thermal (DSC, TGA, DTA), and X-ray diffraction techniques.
- In vitro solubility studies in water, assessment of anti-inflammatory activity in LPS-induced RAW264.7 macrophages, and cytotoxicity evaluation.
Main Results:
- Novel ibuprofen cystamine salts (IBU-CYS 1 and IBU-CYS 2) were successfully synthesized and characterized.
- IBU-CYS 1 and IBU-CYS 2 exhibited significantly improved aqueous solubility (6.11 and 7.81 mg/mL) compared to ibuprofen (0.04 mg/mL).
- In vitro studies demonstrated effective inhibition of inflammatory responses in macrophage cells with no observed cytotoxicity, suggesting therapeutic potential.
Conclusions:
- The synthesized ibuprofen cystamine salts represent a promising approach to overcome the solubility limitations of ibuprofen.
- These novel salts show potential for developing improved pharmaceutical formulations with enhanced bioavailability and anti-inflammatory efficacy.
- Further investigation into hydrogel-encapsulated IBU-CYS2 could lead to advanced drug delivery systems.
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