Influence of Polymer Combınatıon Concentratıon on The Characterıstıcs, In Vıtro Release And In Vıvo Lung Deposıtıon of Algınate-Carrageenan Mıcrospheres Encapsulatıng Cıprofloxacın HCl

Abstract

Inhalation Ciprofloxacin HCl microspheres were formulated with combination of alginate and kappa carrageenan with a total of 1% (F1), 1.5% (F2), and 2% (F3). Aim of this research is to examine effect of polymer concentration on characteristics, release, and lung deposition of microspheres. Microspheres were characterized including loading, efficiency, yield, size, moisture content, mucoadhesivity, and release. Deposition was studied by fluorescence microscopy. Results showed spherical and smooth with size ofless than 2 µm. Loading showed about 18.55% to 29.65%. Entrapment efficiency was 52.86-76.29%. Yield was 49.83-70.72%. Swelling index was less than 10. For moisture content, all formulas demonstrated less than 6.5%. For mucoadhesivity, F1, F2, and F3 showed 0.0090 kg, 0.0217 kg, and 0.0329 kg respectively. It was found that increasing polymer concentration did not affect size, loading, efficiency, and yield of microspheres. Cumulative release at F1, F2, and F3 was 72.64%, 59.25%, and 47.66% respectively in 10 minutes at PBS pH 7.4 with burst release profile. In vivo showed that all formulas were able to deposit on rat lungs and it was found that the intensity were decreased at the 4th hour due to increase of polymer. Remaining intensity indicated that microspheres were able to maintain the drugs loaded.