Abstract:
Background: At present, pharmaceutical researchers are focusing on instantaneous intraoral dispersible technologies as novel drug delivery systems because; they have outstanding advantages over the traditional oral and parenteral routes of drug administration. Some essential natural drugs have low oral bioavailability due to extensive first pass metabolism and pre systemic degradation in the gastrointestinal tract.
Purpose of Study: This research, addresses these problems by formulating a cheap rice paper Intraoral Dispersible Film (IDF). IDFs are effective and could improve the bioavailability of some natural drugs.
Methods: In this study, formulation was optimized using the experimental factorial design. The IDFs were loaded with model, natural, anti-cancer drugs, Resveratrol and Curcumin with low oral bioavailability. They were evaluated for thickness, folding endurance, swelling behaviour, among others. These related to drug release properties. Permeation was evaluated using the pig mucosal membrane mounted on a Franz diffusion cell, and taste testing was done to determine acceptability using a taste panel. Sixteen formulations showed variations in disintegration time, thickness, Tensile strength and permeation profiles.
Results: The key finding is, ex vivo release profiles of the optimized formulation revealed first order release and later zero order. Published results were that When Curcumin was given orally at a dose of 2 g/kg to rats, a maximum serum concentration of 1.35±0.23 µg/ml was observed at time 0.83 hours, whereas in humans the same dose of Curcumin resulted in either undetectable or extremely low (0.006±0.005 µg/ml at 1 hour) serum levels (Siebenand, 2010). Boocock (Boocock et al., 2007) reported Cmax for two separate mono-glucuronide metabolites, for a total glucuronide metabolite concentration ~7.5 µM following a single 5.0 g oral dosage of Resveratrol. In this study, after permeation, a concentration of 6.73mg/ml of Resveratrol and 0.061mg/ml of Curcumin were detected after 2 hours of the experiment after administration of 20 mg of each of the drugs. Conclusions: Therefore, it is evident that rice paper IDF could efficiently deliver natural drugs into the blood.
