Solid lipid microparticles:An approach for improving oral bioavailability of aspirin

The objectives of the work were to develop a lipid based delivery system for aspirin and to evaluate its physicochemical and pharmacodynamic properties.Aspirin-loaded solid lipid microparticles(SLMs)were formulated by hot homogenization and analysed for their encapsulation efficiency(EE%),in vitro release,particle size,anti-inflammatory and ulcer inhibition properties.Particle size ranged from 33.10±5.85 to 43.50±7.27μm for batches A1 to A3 SLMs loaded with 1,3 and 5%aspirin and containing Poloxamer 407,while batches B1,B2 and B3 formulated with Soluplus as surfactant had particle size range of 31.10±1.46 to 45.60±2.92μm.Batches A1 and B1 containing 1%of aspirin had the highest EE of 70 and 72%respectively.Maximum in vitro release of 95.1 and 93.2%were obtained at 8 h from batches A1 and B1 respectively.SLMs exhibited about 77.8%oedema inhibition,while the reference had 66.7%and ulcer inhibition range of 25-75%.Aspirin-loaded SLMs exhibited good properties and could be used orally twice daily for the treatment of inflammation.

Preparation and evaluation of colon targeted drug delivery systems for albendazole using kneading,extrusion and compaction technology

Albendazole is an orally administered broad-spectrum benzimidazole anthelmintic used against helminthiasis,hydatid cyst disease and neurocysticercosis.The objectives of this investigation are to develop a sustained release drug delivery system for albendazole,and to target its delivery to colon.Albendazole matrix tablets containing varying proportions of single and binary blends of four polymers;polyacrylic acid(carbopol 971),ethylcellulose(Etcell),eudragit L100-55(EUD),and sodium carboxymethyl cellulose(CMC) were prepared by a modified wet granulation technique of kneading,extrusion and compaction.In vitro release profiles of albendazole was sequentially determined in simulated gastric fluid(SGF),simulated intestinal fluid(SIF) without enzymes and in rat caecal content medium(RCCM) at 37 ℃.The in vitro drug release from matrix tablets containing CMC and Etcell as single polymers showed initial burst effect in the first 2 h(>20% and 50% respectively),followed by a slow release in SIF.However,matrix tablets containing polymer blends showed that no appreciable drug release occurred up to 5 h.Drug release from tablets containing polymer blends in the dissolution medium containing rat caecal material suddenly increased to ≥30% after 5 h(RCCM),and reaching up to 90% in 24 h.Albendazole matrix tablets containing carbopol 971,Etcell,EUD,and CMC as single polymers and as blends were formulated for oral use.Drug release from the tablet matrices containing carbopol alone,binary blends of carbopol/Etcell,and CMC/EUD were found to be very slow and dependent on polymer concentration.Matrix tablets containing blends of these polymers formulated using kneading,extrusion and compaction technique could provide sustained drug release and can be utilized in the colonic delivery of albendazole.