Development of cross-linked alginate spheres by ionotropic gelation technique for controlled release of naproxen orally

Joshi, Sachi; Patel, Pooja; Lin, S.; Madan, P. L.
February 2012
Asian Journal of Pharmaceutical Sciences;2012, Vol. 7 Issue 1, p134
Academic Journal
Controlled release naproxen spheres were prepared in a cross-linked alginate matrix using ionotropic gelation technique. A suspension of naproxen in 1%, 2%, or 3% w/v sodium alginate solution was added drop wise into 2% w/v calcium chloride solution and the resulting spheres were evaluated for their morphology, physical characteristics, rate of swelling, and micromeritics. Increase in concentration of sodium alginate marginally increased particle size of the spheres. The arithmetic-number mean diameter of naproxen-loaded spheres ranged from 1.09 mm for 1% alginate spheres to 1.31 mm for 3% alginate spheres. The encapsulation efficiency increased linearly with increasing alginate concentration (R² = 0.9996) due to formation of denser spheres. The rate of swelling of the spheres over a 1 h period was about 50% in deionized water and more than 2000% in phosphate buffer solution. The release of naproxen from the spheres studied in phosphate buffer solution (pH 7.4) followed zero-order release kinetics (after the initial burst effect) between 30 and 90 min for 1% and 2% alginate spheres, and between 30 and 120 min for 3% alginate spheres, exhibiting correlation coefficient values ranging from 0.9929 to 0.9999. The rate of release of naproxen decreased with increasing concentration of sodium alginate due to slow penetration of dissolution fluid in the spheres. The results suggest that alginate spheres can potentially deliver naproxen at zero-order controlled release following oral administration.


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