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Development and characterization of naproxen-chitosan solid systems with improved drug dissolution properties.
Paola Mura1, Naima Zerrouk, Natascia Mennini
1Dipartimento di Scienze Farmaceutiche, Facoltà di Farmacia, Università di Firenze, Via Gino Capponi 9, 50121 Firenze, Italy. mura@farmfi.scifarm.unifi.it
Summary
Chitosan enhances naproxen dissolution, especially low molecular weight chitosan (CS-Lw) via cogrinding. This creates stable tablets with improved drug release for fast-acting anti-inflammatory formulations.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
Background:
- Naproxen, a poorly water-soluble anti-inflammatory drug, faces bioavailability challenges.
- Chitosan is an emerging biopolymer with potential pharmaceutical applications.
Purpose of the Study:
- To investigate chitosan's solubilizing and amorphizing properties for naproxen.
- To evaluate different preparation techniques and chitosan molecular weights on drug dissolution.
Main Methods:
- Preparation of solid binary systems using various techniques (mixing, cogrinding, kneading, coevaporation) with different drug/polymer ratios.
- Characterization using phase solubility analysis, DSC, XRD, FT-IR, and SEM.
- Assessment of dissolution properties and tablet compressibility.
Main Results:
- Drug dissolution improved with increased chitosan concentration, optimal at 1:9 (w/w) drug/polymer ratio.
- Low molecular weight chitosan (CS-Lw) was more effective than medium molecular weight (CS-Mw).
- Cogrinding was the most effective technique, increasing naproxen's dissolution rate over tenfold and inducing amorphization.
Conclusions:
- CS-Lw is an optimal carrier for naproxen due to enhanced dissolution, direct compression feasibility, and antiulcerogenic action.
- Fast-release oral solid dosage forms of naproxen can be developed using CS-Lw.
- Cogrinding and optimized drug/polymer ratios are key for improving naproxen's pharmaceutical performance.