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Transport Properties of Ibuprofen Encapsulated in Cyclodextrin Nanosponge Hydrogels: A Proton HR-MAS NMR Spectroscopy Study
Published on: August 15, 2016
Cyclodextrin-based nanosponges encapsulating camptothecin: physicochemical characterization, stability and
Shankar Swaminathan1, Linda Pastero, Loredana Serpe
1Dipartimento di Scienza e Tecnologia del Farmaco, Università degli Studi di Torino, Italy.
Summary
Cyclodextrin nanosponges enhance camptothecin (CAM) solubility and stability, protecting its lactone ring. These novel formulations prolong CAM release and increase its cytotoxicity against cancer cells.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
- Nanotechnology
Background:
- Camptothecin (CAM) is a potent antitumor agent with limited therapeutic use due to poor solubility, lactone instability, and side effects.
- Cyclodextrin-based nanosponges (NS) are advanced drug delivery systems known for improving solubility, protecting active compounds, and controlling release.
Purpose of the Study:
- To formulate camptothecin (CAM) complexes with beta-cyclodextrin nanosponges (NS) using varying cross-linking ratios (1:2, 1:4, 1:8).
- To enhance CAM's lactone ring stability and prolong its release kinetics.
- To evaluate the physicochemical properties and in vitro performance of CAM-loaded NS.
Main Methods:
- Preparation of crystalline and paracrystalline beta-cyclodextrin NS formulations with CAM.
- Characterization using X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC), and Fourier-transform infrared spectroscopy (FTIR).
- Assessment of drug loading, particle size, zeta potential, in vitro drug release, lactone ring stability, and cytotoxicity.
Main Results:
- XRPD, DSC, and FTIR confirmed CAM interaction with NS, with decreased CAM crystallinity.
- Drug loading varied from 13% to 37% w/w in crystalline NS, with lower loading in paracrystalline forms.
- NS formulations demonstrated sustained CAM release over 24 hours, protected the lactone ring (80% intact vs. 20% for plain CAM), and showed enhanced cytotoxicity against HT-29 cells.
Conclusions:
- Beta-cyclodextrin nanosponges effectively encapsulate camptothecin, improving its solubility and stability.
- The developed NS formulations offer a promising strategy for controlled delivery of camptothecin, enhancing its therapeutic potential.
- NS-based camptothecin delivery systems exhibit increased efficacy and reduced degradation under physiological conditions.
