PREPARATION AND EVALUATION OF THE POLYMERIC MICELLAR FORMULATION FOR ORAL DELIVERY OF GRISEOFULVIN
Nanotechnology Research Center, Ahvaz Jundishapur University of Medical Sciences, Ahvaz, Iran
Soror Khodarahmpour
School of Pharmacy, Ahvaz Jundishapur University of Medical Sciences, Ahvaz, Iran.
Anayatollah Salimi
School of Pharmacy, Ahvaz Jundishapur University of Medical Sciences, Ahvaz, Iran.
Many of drugs have poor water solubility and so the oral delivery of such drugs is usually associated with limitation of low bioavailability and lack of dose proportionality. Micellar systems are excellent potential formulation for increasing solubilization and bioavailability of drugs. The aim of this study was to formulate polymeric micellar containing a lipophilic drug, griseofulvin, and to explore the potential of carriers for such system. Full factorial design with three variables; drug concentration, type of surfactant mixture and cosurfactant concentration in two levels were used. The effects of variables on formulation characters; particle size, drug release and rat intestine permeability were evaluated. All formulations with particle size between 74.33 to 220 nm significantly increased griseofulvin aqueous solubility that this effect is dependent to surfactant mixture. The results showed oleic acid as oil, labrafil with labrasol and Poloxamer and propylene glycol as surfactant mixtures, capryol 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 (%D24) was between 4.59 to 42.41, that minimum and maximum of % D24, belongs to formulation No.7 and 2 respectively. All polymeric micellar formulations increased drug permeated through rat intestine. Maximum increase in p4 was 20.5-folds compare to control. The result shows that Drug permeability through rat intestine did not influence by type of surfactant and only controlled by percent of drug that is loaded in this manner that higher permeability performed with lower drug amount
4 , 2 , 2014
92 - 97
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