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Updated: Jul 6, 2026
10:10
Transport Properties of Ibuprofen Encapsulated in Cyclodextrin Nanosponge Hydrogels: A Proton HR-MAS NMR Spectroscopy Study
Published on: August 15, 2016
Microspheres for colonic delivery of ketoprofen-hydroxypropyl-beta-cyclodextrin complex
F Maestrelli1, N Zerrouk, M Cirri
1Department of Pharmaceutical Sciences, University of Florence, via Schiff 6, 50019 Sesto Fiorentino, Florence, Italy. francesca.maestrelli@unifi.it
Summary
This study developed novel microspheres for colon-specific drug delivery using ketoprofen. The system enhances drug permeation and shows safety, indicating potential for improved therapeutic outcomes.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Materials Science
Background:
- Developing colon-specific drug delivery systems is crucial for treating colonic diseases.
- Ketoprofen, a non-steroidal anti-inflammatory drug, requires effective delivery systems to maximize efficacy and minimize side effects.
- Multiparticulate systems offer advantages in controlled and targeted drug release.
Purpose of the Study:
- To develop a novel multiparticulate system for site-specific colon delivery of ketoprofen.
- To investigate the synergistic effects of cyclodextrin complexation and chitosan-based microspheres on drug solubility, release, and permeation.
- To evaluate the safety and efficacy of the developed drug delivery system.
Main Methods:
- Ketoprofen was complexed with hydroxypropyl-beta-cyclodextrin (HPbetaCyd) and formulated into calcium pectinate and chitosan microspheres (MS).
- Drug entrapment efficiency, release kinetics, and permeation across Caco-2 cells were assessed.
- Solid-state interactions were analyzed using FTIR, DSC, and X-ray diffraction; morphology was examined by SEM.
Main Results:
- Microspheres demonstrated varied drug release profiles based on cyclodextrin complexation and chitosan presence, influenced by reservoir and competition effects.
- Drug permeation across Caco-2 cells was significantly enhanced by the microsphere formulation, especially when ketoprofen was complexed with HPbetaCyd, showing a synergistic effect with chitosan.
- Cytotoxicity tests confirmed the safety of the developed formulations.
Conclusions:
- The developed multiparticulate system effectively improves ketoprofen solubility and enhances its permeation, showing significant potential for colon-specific drug delivery.
- The combination of cyclodextrin complexation and chitosan-based microspheres offers a synergistic approach to optimize drug delivery and therapeutic efficacy.
- This novel system represents a promising strategy for improving the treatment of colonic inflammatory conditions.
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