Abstract
The objective of this study was to investigate the influence of type of cross-linking method used on the properties of ambroxol hydrochloride microspheres such as encapsulation efficiency, particle size, and drug release. Microspheres were prepared by solvent evaporation technique using chitosan as a matrix-forming agent and cross-linked using formaldehyde and heat treatment. Morphological and physicochemical properties of microspheres were then investigated by scanning electron microscopy (SEM), X-ray diffractometry (XRD), differential scanning calorimetry (DSC), and Fourier-transform infrared spectroscopy (FTIR) spectroscopy. The cross-linking of chitosan takes place at the free amino group because of formation of imine bond as evidenced by FTIR. The DSC, XRD, and FTIR analysis showed that chitosan microspheres cross linked by heating were superior in properties and performance as compared to the microspheres cross-linked using formaldehyde. SEM results revealed that heat-treated microspheres were spherical, discrete having smooth, and porous structure. The particle size and encapsulation efficiencies of the prepared chitosan microspheres ranged between 10.83–24.11 μm and 39.73μ80.56%, respectively. The drug release was extended up to 12 h, and the kinetics of the drug release was obeying Higuchi kinetic proving diffusion-controlled drug release.
Highlights
Ambroxol is an active N-desmethyl metabolite of the mucolytic bromohexine
Microspheres were prepared with varying ratios of chitosan: drug like 1:1, 2:1, 3:1, and 4:1 and designated as, FA-1, FA-2, FA-3, and FA-4, respectively. (b) To produce the heat treatment cross-linked chitosan microspheres, the temperature of the emulsion was raised up to 60°C and stirred at 500 rpm overnight
This study was undertaken to evaluate the effect of the method of cross-linking onto the performance of chitosan microspheres
Summary
Ambroxol is an active N-desmethyl metabolite of the mucolytic bromohexine. It is indicated for acute and chronic. Journal of Young Pharmacists Vol 3 / No 1 disorders of respiratory tract, where there is copious thick secretion or mucus production. It has biological half-life of 3–4 h. To reduce frequency of dosing as well as to increase bioavailability and enable better patient compliance, formulating sustained release dosage form was necessary.[1,2,3,4] Several sustained release formulations of ambroxol hydrochloride have been reported.[5,6,7]
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