Preparation and properties for magnetic/pH double sensitive hydrogel beads carrying carbamazepine / 中国组织工程研究

ABSTRACT

BACKGROUND:The faults or defects in pharmaceutical dosage form designed for carbamazepine may lead to irregular drug absorption, great individual differences between the pharmacokinetics, narrow therapeutic concentration range, and the therapeutic drug monitoring for this drug. OBJECTIVE:To prepare a magnetic/pH double sensitive hydrogel beads carrying carbamazepine and to evaluate its properties. METHODS:Using chitosan, alginate and Fe3O4 nanoparticle as carrier materials, the magnetic/pH double sensitive hydrogel beads carrying anti-epileptic carbamazepine were prepared, and the composition and preparation technology were optimized by orthogonal test of L9(34). The surface morphology and structure of the hydrogel beads were characterized by scanning electron microscopy and Fourier transform infrared spectroscopy respectively. Also, the superparamagnetism, swel ing and release in vitro of hydrogel beads were determined. RESULTS AND CONCLUSION:The optimized preparation technology were described as0.5%(w/v) chitosan, 1.5%(w/v) alginate, 2.0%(w/v) calcium chloride, and 12 ratio for magnetic versus carrier materials. The hydrogel beads under the optimal preparation conditions showed a round shape and smooth surface, and average encapsulation efficiency, loading efficiency and hydrogel beads diameter were 94.36%, 25.05%and 1-2 mm respectively. The hydrogel beads appeared to have superparamagnetism, the swel ing degrees were associated with pH value of medium, and the sequential release amount of carbamazepine from the hydrogel beads in simulated gastric fluid was 22.77%for 2 hours. Then, the beads were moved to the simulated intestinal fluid, and this value approached 91.63%for 24 hours. Experimental findings indicate that, the composition and preparation technology of magnetic/pH double sensitive hydrogel beads carrying carbamazepine was rational and feasible, and hydrogel beads show obvious pH sensitivity and magnetic sensitivety. The control ed-release effect of hydrogel beads in vitro is also good.