ABSTRACT
This study describes the formulation of bioadhesive buccal gels for fluconazole delivery via buccal mucosa. In the present study the polymer with well-defined mucoadhesive properties like Carbopol 934 was used. Carbopol- Poloxamer gels of 1% fluconazole was formulated with various absorption enhancers like polyethylene glycol, propylene glycol, glycerol, phosphatidylcholine, mannitol and sodium lauryl sulphate by cold method. The gels were characterised for gelation temperature, bioadhesive force, pH, viscosity, drug release profile, ex vivo permeation across goat buccal mucosa and stability profile. The percent drug permeated through the buccal mucosa was in the range of 62-76%. Polyethylene glycol and propylene glycol were found to be better absorption enhancers as compared to others and followed zero order release kinetics.
ABSTRACT
The objective of the present study was to develop and evaluate bioadhesive buccal patches for mucosal delivery of diltiazem. The antihypertensive agent, diltiazem, undergoes first pass metabolism which compromises its bioavailability and the buccal route is a viable alternative to bypass this metabolism. In the present study, the buccal patches were fabricated with Eudragit L100 as the film forming polymer and hydroxypropyl methylcelluose, Carbopol 934 and sodium carboxymethylcellulose as the mucoadhesive polymer. The patches were characterized for various physicochemical attributes viz., weight uniformity, surface pH, folding endurance, swelling profile, content uniformity, permeability study, in vitro drug release profile and stability study in saliva. The results indicate that the Carbopol 934 is suitable for fabricating buccoadhesive patches with requisite release and stability profile.
ABSTRACT
The aim of the present work was to develop drug delivery system for localized controlled release of metronidazole following insertion into and/or around the periodontal pocket. This would ensure increased local drug concentration at the periodontal site to maintain an effective concentration over an extended period of time and a decrease in superfluous distribution of the drug to other body organs with a subsequent decrease in side effects. In the present work, metronidazole loaded chitosan microspheres were prepared by external gelation technique using tripolyphosphate as the cross-linker. The drug to polymer ratio was chosen at three levels: 1:4, 1:5 and 1:6 (by weight) and tripolyphosphate concentration also at three levels: 6, 12 and 18 (%). The microspheres were characterized for surface morphology, particle size, drug entrapment efficiency, swelling, erosion, bioadhesion and drug release profile. Nearly spherical, rough and porous particles (size ~ 800 μm) were obtained. Drug entrapment efficiency was found to be in the range of 60-75%. Percentage swelling, erosion and bioadhesion ranged from 10-25%, 5-15% and 43-59% respectively. The results indicated that formulation of metronidazole in chitosan microspheres could be utilized as a potential drug delivery system to periodontal pocket.