In vitroandin vivostudies of ibuprofen-loaded biodegradable alginate beads

Abstract

The irritation effects of ibuprofen, a widely used non-steroidal anti-inflammatory drug (NSAID), were evaluated on mouse gastric and duodenal mucosa when suspended in 0.5% (w/v) sodiumcarboxymethylcellulose (NaCMC) solution and loaded in alginate beads. The ionotropic gelation method was used to prepare controlled release alginate beads of ibuprofen. The influence of various formulation factors on the encapsulation efficiency, as in vitro drug release and micromeritic properties, was investigated. Other variables included the alginate concentration, percentage drug loading and stirring speed during the microencapsulation process. Scanning electron micrographs of alginate beads loaded with ibuprofen showed rough surface morphology and particle sizes in the range of 1.15 +/- 0.4 - 3.15 +/- 0.6 mm. The yield of microspheres, as collected after drying, was generally 80-90%. Formulation code H showing t50% value of 3.5 h was chosen for in vivo trials because of the appropriate drug release properties. For in vivo trials, free ibuprofen (100 mg kg(-1)), blank and ibuprofen (100 mg kg(-1)) loaded alginate beads (formulation code H) were suspended in 0.5% (w/v) NaCMC solution and each group was given to six mice orally by gavage. NaCMC solution was used as a control in experimental studies. In vivo data showed that the administration of ibuprofen in alginate beads prevented the gastric lesions.

Hydrogels of Dextran Containing Nonsteroidal Anti-Inflammatory Drugs as Pendant Agents

“…To reduce gastrointestinal symptoms and prolong drug activity, NSAIDs are often formulated as modified delivery systems, such as enteric-coating or sustainedrelease methods. The research of systems more efficient than those already present on the market continuously increases, and this trend is confirmed by the relevant number of patents and papers reported in the literature in the past year (Arica et al;Freitas and Marchetti;Landgraf, Li, and Benson 2005).…”

Alginate microspheres obtained by the spray drying technique as mucoadhesive carriers of ranitidine

“…-RNT loading in the microspheres was determined by dissolving an accurately weighed amount of microspheres (20 mg) in 10 mL distilled water and agitating it for 24 h at 150 rpm in a water bath (15). A er fi ltration through a 0.45-mm cellulose acetate Millipore fi lter (Millipore), RNT concentration was determined by HPLC.…”

Encapsulation and release characteristics of glibenclamide loaded calcium-alginate beads

“…Encapsulation efficiency was 70%, which could be considered satisfactory; however, this result suggests analyzing the variables that may be reducing the effectiveness of the beads (time and agitation speed, contact time with calcium chloride, and the concentration of solutions) because Arica et al reported an efficiency of 80-90%. 30 Additionally, stability of glibenclamide in loaded calcium-alginate beads was evaluated by determining content of drug by HPLC method at 3, 6, 9 and 12 months ( Table 3). The data show a stable formulation.…”

“…Solutions were pre-treated and maintained at 37 ± 0.5 ºC and the paddles were set at 75 rpm. At appropriate time intervals (10,20,30,45 and 60 min), 5 mL samples were collected, filtered through 0.45 μ filter paper and analyzed for drug content by HPLC at 230 nm. An equal volume of fresh medium was added to the test solution to maintain constant volumes.…”