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Paper Details

FORMULATION AND EVALUATION OF POLYMERIC MICELLE DRUG DELIVERY SYSTEM OF CELECOXIB TO IMPROVE THE ORAL ABSORPTION

Anayatollah Salimi*1, Behzad Sharif Makhmal Zadeh1, Najme Mahmoudabadi1
Abstract


Purpose: The aim of this study was to formulate polymeric micelle systemcontaining a lipophilic drug, celecoxib, and to explore the potential of carriers for such system. Methods: Full factorial design with three variables; drug percentage, type of surfactant mixture and co surfactant amount in two levels were used. The effects of variables on formulation characters; particle size, drug release and permeability from rat intestine were evaluated. Results: All formulations with particle size between 7.63 to 97.66 nm significantly increased celecoxib aqueous solubility that this effect is dependent to surfactant mixture. The results showed oleic acid as oil, labrafil -labrasol and Poloxamer - propylene glycol as surfactant mixtures, Capryol 90 as co-surfactant and lecithin as oily phase and membrane stabilizer agent prepared stable micellar formulations with sustained release property. Percent of drug release after 24 hrs. (% DR24) was between 11.95 to 46.82. All polymeric micelle formulations increased drug permeated through rat intestine. Maximum increase in p4 was 39.12 times compared to control. The result shows that drug percent and co surfactant amounthave a significant relationshipwith % P4. (p?0.05). All drug formulations containing 3% of drug, as compared to formulations containing 1% have a higher rate of gastrointestinal absorption. Conclusion: All formulations indicated sustained release profiles. Drug permeability through rat intestine was controlled by percent of drug and co surfactant amount in formulations so that higher permeability resulted with higher drug percent and lower co surfactant amount. This finding may be suggested un saturated intestine absorption of celecoxib.

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