Formulation And Evaluation Of Taste-Masked Ciprofloxacin ...

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IJPFR, Oct-Dec 2012; 2(4):-45-59 Original article ISSN 2249 – 1112 46 concentrations at the site over the course of the treatment period. Moreover, systemic antibiotic therapy carries with it the risk of the host developing resistance. Due to these negative effects, the use of local drug delivery devices containing antibiotics which can maintain therapeutic concentrations at the site of infection is an approach that may be explored. This could enhance the therapy of periodontal diseases while also reducing side effects (1-4). Ciprofloxacin is a second generation fluroquinolone derivative, exhibiting activity against a wide range of Gram-negative and Gram-positive facultative bacteria as well as periodontal pathogens (5). Mucoadhesive polymers are the important component in the development of buccal delivery system. These polymers enable retention of dosage form at the buccal mucosal surface and thereby provide intimate contact between the dosage form and the absorbing tissue (6). Chitosan is a hydrophilic biopolymer obtained by alkaline deacetylation of chitin, a major component of arthropod shells, and possesses favorable properties such as nontoxicity, biocompatibility, bioadhesivity and biodegradability. Moreover, chitosan itself possesses antimicrobial activity (7-8). Therefore the aim of this work was to develop taste-masked ciprofloxacin bioadhesive dental films for the treatment of periodontal pathogens diseases. EXPERIMENTAL Materials Ciprofloxacine was kindly supplied by Elpharonia company, Egypt, Sodium Saccharine was purchased from LOBA CHEMIE PVT. LTD. (INDIA), Chitosan low molecular weight was kindly supplied by sigma Pharmaceuticals (Cairo, Egypt), Hydroxypropyl methylcellulose (hydroxypropyl (12wt%), Methoxy (28wt%)), (Fluka-Biochemica, Switzerland). -Carbopol 934 (Luna Co. from Bf.Goodrich, USA). All water used was distilled de-ionized water. All other chemicals were of reagent grade and used as received. Equipment -Digital electric balance (Mettler), (India)- pH meter (CG 820 Schott-Gerate, W. Germany)-Thermostatically controlled magnetic stirrer (Philip Harris Ltd), (Shenstone, England)-Differential Scanning Calorimeter, Shimadzu, model DSC-50, (Japan)-Infrared Spectrophotometer (Shimadzu IR-4351, Shimadzu, Japan)-Tensile strength machine (Chatillon Force Measurment- Greensbora, NC27409, India)- Dissolution apparatus II, (Hanson Research, SR8 plus, Dissolution Test Station, USA)-Spectrophotometer, (Shimadzu, model UV-1601, Japan)-Oven, Fisher isotemp oven, 200 series, model 230F, (USA), scanning electron microscope (SEM), (JSM- 6360L, V 1 Japan. Methodology Preformulation study Preparation of ciprofloxacin-saccharinate complex A molar solution of ciprofloxacin in 0.1 N acetic acid was mixed with aqueous molar solution of saccharin sodium. The mixture was stirred for 15 minutes using magnetic stirrer and the obtained ciprofloxacin-saccharinate complex was separated by filtration, air dried and kept in desiccator. Characterization of ciprofloxacin-saccharinate complex 1- Microscopic examination: Soliman et al © 2012 International Journal of Pharmaceutical Frontier Research
IJPFR, Oct-Dec 2012; 2(4):-45-59 Original article ISSN 2249 – 1112 47 Scanning electron microscope (SEM) was used to examine the shape of the produced ciprofloxacin saccharinate complex and compare it with ciprofloxacin raw material. In addition, photomicrographs of them were taken. 2- UV-scanning and calibration curve in different media: Ciprofloxacin and ciprofloxacin saccharinate complex solutions in 5% acetic acid and phosphate buffer pH 6.8 were scanned spectrophotometerically using UV spectrophotometer. The λmax for each solution was determined. Serial concentrations of the drug and its complex in both solvents were prepared. The absorbance of the prepared solutions was measured spectrophotometerically at the predetermined λmax. The measured absorbance was plotted against the corresponding concentrations and the procedural constant (K) was calculated from the measured data corresponding to the best fitting straight line. 3- Solubility determination Solubility determination of ciprofloxacin and its complex in 5% acetic acid and phosphate buffer pH 6.8 using vial and shaker method were done. An excess amount of the powder was added in sealed glass vial in presence of 3 ml of each solvent, these vials were shacked for 24 hours at room temperature then the contents of each vial were filtered and the filtrate was diluted and measured spectrophotometerically. 4- Determination of the actual drug content in the complex: The actual drug content in the complex was calculated by dissolving certain amount of the drug and its complex in 100 ml phosphate buffer pH 6.8, the absorbance of each was measured spectrophotometrically and the drug content was calculated using the previously constructed calibration curve. 5- Fourier transform infrared (FTIR) analysis: Infrared absorption spectra of ciprofloxacin and ciprofloxacin-saccharinate complex were recorded using a FTIR spectrometer. Spectral scanning was conducted from 4000 to 400 cm −1 at a resolution of 4 cm −1 of fresh samples (weighing approximately 4 mg) that compressed into discs using KBr. 6- Differential scanning calorimetric (DSC): The thermal behaviors of ciprofloxacin and ciprofloxacin-saccharinate complex were recorded using a differential scanning calorimeter after calibration with indium and lead standards. Pre-weighed samples (4 mg) were heated in crimped aluminum pans in an atmosphere of nitrogen. Samples were heated at a constant heating rate of 10°C/min over a temperature range of 25–300°C. Formulation of ciprofloxacin-saccharinate bioadhesive films Preparation of the films Ciprofloxacin saccharinate films were prepared using 2% chitosan in 5% acetic acid solution alone and with carbopol 934 and HPMC in different concentrations as shown in table 1. The films were prepared by solvent casting technique (9). The predetermined amounts of chitosan and other polymers were soaked in 50 ml 5% acetic acid solution, then determined amount of cipro-saccharine complex (equivalent to 250 mg cipro), and plasticizer (5%w/v glycerin) were added. The mixture was stirred with the aid of mechanical stirrer to ensure complete drug and plasticizer distribution, this solution was taken and poured in dry glass Petri -dish (10 cm diameter) and dried at room temperature. After complete drying, films were cut into pieces (2*2 cm) and kept in aluminum foil. Soliman et al © 2012 International Journal of Pharmaceutical Frontier Research
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Formulation And Evaluation Of Taste-Masked Ciprofloxacin ...

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