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Influence of hydroxypropyl-beta-cyclodextrin complexation on piroxicam release from buccoadhesive tablets
Mario Jug1, Mira Bećirević-Laćan
1Department of Pharmaceutics, Faculty of Pharmacy and Biochemistry, University of Zagreb, A. Kovacića 1, 10 000, Zagreb, Croatia. mira_becirevic@Yahoo.com
Summary
Hydroxypropyl-beta-cyclodextrin (HPbetaCD) forms an inclusion complex with piroxicam (PX), enhancing its release from controlled-release tablets. This complexation improves drug solubility and diffusion, leading to faster drug delivery.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Physical Chemistry
Background:
- Piroxicam (PX) is a sparingly water-soluble non-steroidal anti-inflammatory drug.
- Cyclodextrins, particularly hydroxypropyl-beta-cyclodextrin (HPbetaCD), are widely used to improve the solubility and bioavailability of poorly soluble drugs.
- Controlled-release drug delivery systems aim to provide sustained drug release and improve patient compliance.
Purpose of the Study:
- To investigate the interaction between piroxicam (PX) and hydroxypropyl-beta-cyclodextrin (HPbetaCD) in both solution and solid states.
- To prepare and characterize PX-HPbetaCD inclusion complexes.
- To evaluate the effect of HPbetaCD complexation on the release of PX from buccoadhesive controlled-release tablets formulated with hydrophilic polymers.
Main Methods:
- Solubility studies to determine stoichiometry of PX-HPbetaCD complexation.
- Characterization of solid systems using differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR), and X-ray diffractometry (XRD).
- Preparation and evaluation of buccoadhesive controlled-release tablets using hydroxypropylmethyl cellulose (HPMC) and Carbopol 940 (C940), assessing dissolution, swelling, and mucoadhesive properties.
Main Results:
- PX-HPbetaCD inclusion complex formation with 1:1 stoichiometry was confirmed.
- Solid-state characterization confirmed the formation of the inclusion complex.
- Tablets containing the PX-HPbetaCD solid complex exhibited faster piroxicam release compared to physical mixtures or free drug.
- Differences in release rates were attributed to polymer properties and cyclodextrin complexation, affecting drug solubility and diffusivity.
Conclusions:
- HPbetaCD effectively forms an inclusion complex with PX, enhancing its solubility.
- The PX-HPbetaCD complexation significantly modifies the release profile of piroxicam from hydrophilic matrices.
- Buccoadhesive tablets formulated with HPbetaCD complex show improved drug release characteristics, offering potential for enhanced drug delivery.