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Abstract

CATECHIN LOADED CHITOSAN NANOPARTICLES AS A NOVEL DRUG DELIVERY SYSTEM FOR CANCER – SYNTHESIS AND IN VITRO AND IN VIVO CHARACTERIZATION

Rajalakshmi Manikkam*, Daisy Pitchai

ABSTRACT

Aim: The major thrust area in drug discovery research is the designing of a better delivery system that are capable of delivering drugs to the right place, at appropriate time and at required dosage. One such delivery system is drug loaded nanoparticles. Recently, plant derived compounds have taken a main role in ameliorating human diseases. Catechin a flavanoid, is one such compound possessing a broad spectrum of therapeutic efficacy. To improve these efficacies further, the present study was aimed to load catechin into polymeric nano particles and evaluate its anticancer property. Materials and Methods: Catechin was isolated using bio-assay guided fractionation from the methanolic extract of Cassia fistula. Catechin was loaded into the chitosan-alginate and chitosan-carrageenan nanoparticles by ionotropic pre-gelation of an alginate/carrageenan core followed by chitosan polyelectrolyte complexation. Morphology and structure characterization of nanoparticles were investigated by scanning electron microscope (TEM) and Fourier transform infrared spectra (FTIR), respectively. The diameter of the nanoparticles was about 20-50 nm, suitable for uptake within the gastrointestinal tract due to their nanosize range and mucoadhesive properties. In addition, the drug encapsulation efficiency, loading capacity, muco-adhesive strength, stability at various temperatures, swelling behaviour, in-vive bio-distribution and drug deposition in plasma and tissues after oral administration for 15 days were studied. The therapeutic efficacy against cancer was evaluated on human prostate cancer cell lines through MTT assay. Results: The results of these studies reveals that, the polymers are muco-adhesive in nature that could have good encapsulation efficiency(65%-97%), provide long stability for catechin(99.56%-94.5%), cause a sustained release of catechin and cause a better bio-distribution and catechin deposition in plasma and tissues. In addition the catechin loaded nanoparticles was found to be non toxic and was found to possess anticancer activity. Conclusion: These results reveal that chitosan –alginate polymeric nanoparticles are better than the chitosan-carrageenan nanoparticles. Catechin loaded nanoparticles provides an opportunity to expand the clinical repertoire of this efficacious agent by enabling ready aqueous dispersion.

Keywords: Chitosan, alginate, carrageenan, nanoparticles, drug delivery, catechin, muco-adhesive, in-vivo biodistribution, anti cancer activity, catechin loaded nanoparticles.


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