Retno Sari and Aty Widyawaruyanti and Franciscus B. Tedy Anindita and Sinta Kusuma Astuti and Dwi Setyawan (2018) Development of andrographolide - carboxymethyl chitosan nanoparticles: characterization, in vitro release and in vivo antimalarial activity study. Turkish Journal of Pharmaceutical Sciences, 15 (2). pp. 136-141.

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Abstract

Objectives: The purpose of this study was to investigate the effect of andrographolide-carboxymethyl chitosan nanoparticles formation on the physical characteristics, in vitro release profile and in vivo antimalarial activity of andrographolide. Materials and Methods: Nanoparticles were prepared by ionic gelation method-spray drying using CaCl as the crosslinker with a composition of drug: polymer: CaCl2 2=40: 250: 100. The obtained particles were evaluated for its size and morphology; physical state, drug content, in vitro drugrelease and in vivo antimalarial activity on Plasmodium berghei infected mice. Results: The results of DTA and XRD showed that nanoparticle systems had a lower melting point and lower crystallinity degree. The drug dissolved from the nanoparticles was increased up to 6.5 times and the in vivo antimalarial activity was 1.65 times higher compared to andrographolide. Conclusion: The formation andrographolide-carboxymethyl chitosan nanoparticles affected the physical characteristics of andrographolide. The decrease crystallinity of andrographolide resulted in a lower melting point of andrographolide. Such changes provided a positive impact to the drug dissolution and then its activity. Key words: Andrographolide, carboxymethyl chitosan, in vitro release, in vivo antimalarial, ionic gelation, spray drying

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