Rutaecarpine found to have anti cancer properties. The compound is well-tolerated with low toxicity profile but its
clinical translation against cancer is limited due to poor dissolution characteristics, and substantial first-pass metabolism.
Objective: This paper deals with the preparation, optimization and characterization of Chitosan nanoparticles encapsulating
Rutaecarpine for its intended use as anticancer formulation. Methods:. A number of variables such as organic solvent, its ratio
with aqueous phase, drug to polymer ratio, mixing speed were optimized. To investigate the effect of process variables on mean
particle size, drug loading and entrapment efficiency of several stabilizers were also screened. In vitro Rutaecarpine release was
studied using dialysis bag method. Final formulation was freeze dried for long term storage for which a number of lyoprotectants
were screened. Results: It was observed that stabilizer, solvent, drug to polymer ratio, surfactant concentration, organic/aqueous
phase volume ratio and stirring speed influence nanoparticle size significantly whereas drug loading and entrapment efficiency
were significantly influenced by stabilizers, solvents, drug to polymer ratio and surfactant concentration. Optimized parameters
were chitosan and TPP concentration 0.5 mg/ml, chitosan to TPP ratio 4:1, magnetic stirring at 1000 rpm just for five minutes
was found to be sufficient.. So, based on in vitro characterization and lyophilization of all the Rutaecarpine nanoparticulate
formulations based on natural biodegradable polymers, folic acid coated chitosan nanoparticles were found to be the best for
encapsulation of Rutaecarpine and was selected for in vitro anticancer study.
Key words: PLA, Rutaecarpine, polymeric nanoparticles, emulsification solvent diffusion method.
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