e -Issn : 0976 - 3651
Print-Issn : 2229-7480

  ABSTRACT

FORMULATION AND EVALUATION OF CAPECITABINE NANOPARTICLES FOR CANCER THERAPY

The main objective of this study is to formulate the Capecitabine loaded nanoparticles of chitosan (CS) cross-linked with Tripolyphosphate (TPP) for anti-cancer therapy, inorder to enhance bioavailability and to reduce dose frequency. Formulation of capecitabine loaded CS/TPP nanoparticles solution was prepared by dissolving chitosan (CS) in 1% (w/v) acetic acid solution under stirring at room temperature. The CS solution was diluted with deionized water to produce different concentration. CS/TPP nanoparticles were prepared according to the ionotropic gelation process. For preparation of Capecitabine loaded CS/TPP nanoparticles, the capecitabine solution with various concentrations was added slowly to CS solution and TPP solution was added drop wise to the mixture with mild stirring for 60 min. The prepared nanoparticles were characterized by FT-IR spectroscopy to confirm the cross linking reaction between CS and cross linking agent. X-ray diffraction was performed to reveal the crystalline nature of the drug after encapsulation. Capecitabine were loaded into the nanoparticles and the average size was found to be in the range of 120-250 nm. The Polydispersity index of the nanoparticles was found to be 0.200-0.400. The nanoparticles formed were spherical in shape with high zeta potentials (higher than +20 to +32). In vitro release studies in phosphate buffer saline (pH 7.4) showed an initial burst effect and followed by a slow drug release. The drug release followed zero order kinetics and a Fickian transport mechanism. From all these results it is concluded that the six formulations are recommended for future studies like Nano dry powder preparation. Drug loading capacity was determined by UV spectrophotometer at 240nm. The formulation was optimized for their particle size, drug release and entrapment efficiency for three independent variables by Box-Bekhen design.

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