Gastro-retentive floating beads of curcumin β-cyclodextrin complex to treat stomach tumors

Abstract

The aim of present study was to develop a multi-unit gastro-retentive floating dosage form of curcumin with targeted and sustained release characteristics. Although, protective effect of curcumin against inflammation and cancer is well documented, the clinical potential is underutilized owing to the physicochemical properties of the molecule which lead to poor oral bioavailability. Aqueous solubility of curcumin was enhanced by complex formation with β-cyclodextrin (β-CD). This complex with enhanced solubility profile was further used to prepare multiple unit floating beads. Floating beads of curcumin β-cyclodextrin complex (FBCC) were prepared by dripping a mixture of sodium alginate and hydroxypropyl methylcellulose solution into calcium chloride solution acidified with acetic acid. FBCC were evaluated for percent drug entrapment, diameter, surface topography, buoyancy,<em> in vitro</em> release and pharmacodynamic activity against Benzo(a) pyrene [B(a)P] induced forestomach papillomas in albino female mice (Balb/C strain). The investigation revealed that floating beads possessed optimum formulation characteristics. The drug release from FBCC was fickian and sufficiently sustained for 12 h. Results of antitumor studies against B(a)P induced neoplasia of forestomach suggests that the tumor incidence significantly reduced (50%) using FBCC where as pure curcumin resulted in only 25% reduction. A multi-unit floating dosage form of curcumin β-CD complex possessing sustained release characteristics was developed for targeting gastric tumors. Results of i<em>n vitro</em> studies and anti-tumor studies in animals suggest that FBCC can be safely and effectively used to treat neoplasia of stomach. However, these preliminary investigations warrant further pharmacokinetic studies and clinical evaluation in humans