Abstract
Purpose: To formulate carbomer gel to localize and target drug action in periodontal pockets. Methods: Diclofenac sodium (DS, anti-inflammatory) and metronidazole hydrochloride (MH, antibacterial) were loaded in gelatin microspheres using glutaraldehyde cross-linking. The microspheres were evaluated for drug loading, entrapment and encapsulation efficiency, particle size, drug release as well as by scanning electron microscopy (SEM) and differential scanning calorimetry (DSC). The microspheres were incorporated into carbomer gel and evaluated for drug release. Results: Loading, entrapment and encapsulation efficiencies of DS in the microsphere were 23.4, 93.6, and 74.9 w/w%, respectively, while for MH the values were 21.5, 86.0 and 73.1 % w/w, respectively. Mean particle size of unloaded microspheres, DS- and MH-loaded microspheres was 33.5, 67.8 and 51.4 µm, respectively. SEM showed spherical geometry of microspheres while DSC indicated the amorphous nature of t entrapped DS and MH. Sustained release of DS and MH over a 4-h period from the microspheres and gel was achieved. Conclusion: Carbomer gel loaded with microspheres of diclofenac and metronidazole is a potential localized delivery system for the treatment inflammation and infection in periodontal pockets.
Highlights
Periodontitis is an inflammatory disease caused by chronic bacterial infection of the gum and bone supporting the teeth [1,2]
Since the preparation has the same base at the time of administration, gel containing diclofenac sodium and metronidazole can be mixed and applied to the periodontal cavity with a special dispenser [4] used by the periodontist to deliver medication or gel formulation into periodontal pockets
To overcome problems associated with the conventional system, we aimed to develop a bioadhesive gel formulation which can sustain and localize the drug in the periodontal pockets for an effective treatment
Summary
Periodontitis is an inflammatory disease caused by chronic bacterial infection of the gum and bone supporting the teeth [1,2]. Non-steroidal anti-inflammatory drugs (NSAIDs) such as ibuprofen and diclofenac sodium are used to treat pain and inflammation These drugs are administered locally as gel or given orally in the form of tablets. Due to their short half life, these medications have to be taken frequently to maintain the desired therapeutic effect. In periodontal diseases, both drugs are used simultaneously to treat infection and inflammation. Since the preparation has the same base at the time of administration, gel containing diclofenac sodium and metronidazole can be mixed and applied to the periodontal cavity with a special dispenser [4] used by the periodontist to deliver medication or gel formulation into periodontal pockets
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