In vitro and in vivo studies of ibuprofen-loaded biodegradable alginate beads.
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.
Arica
B
B
Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Hacettepe, Ankara, Turkey.
Caliş
S
S
Atilla
P
P
Durlu
N T
NT
Cakar
N
N
Kaş
H S
HS
Hincal
A A
AA
D000464:Alginates; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology*; D001672:Biocompatible Materials; D001673:Biodegradation, Environmental; D002266:Carboxymethylcellulose Sodium; D003692:Delayed-Action Preparations / Q000494:pharmacology; D004339:Drug Compounding / Q000379:methods*; D004386:Duodenum / Q000187:drug effects; D005260:Female; D005753:Gastric Mucosa / Q000187:drug effects; D007052:Ibuprofen / Q000494:pharmacology*; D007413:Intestinal Mucosa / Q000187:drug effects; D051379:Mice; D008855:Microscopy, Electron, Scanning / Q000379:methods; D008863:Microspheres; D010316:Particle Size; D013499:Surface Properties
D000464:Alginates; D000894:Anti-Inflammatory Agents, Non-Steroidal; D001672:Biocompatible Materials; D003692:Delayed-Action Preparations; D002266:Carboxymethylcellulose Sodium; D007052:Ibuprofen