Antimalarial Activity of Bidens pilosa Root Extract Co-spray Dried in the Presence of β-Cyclodextrin or Aerosil:Microcrystalline Cellulose Blend

Abstract

The purpose of this work was to evaluate if the antimalarial activity of Bidens pilosa L. root extract could be enhanced by co-spray drying with the pharmaceutical excipients blend of colloidal silicon dioxide:microcrystalline cellulose and β-cyclodextrin. The in vivo antimalarial activity of the products was evaluated in mice infected with Plasmodium berghei. Acute in vivo and in vitro toxicity in S5 HeLa cells were also carried out. B. pilosa L. root extract was lyophilized and used as a control. The spray-dried preparations enhanced the survival of the infected mice compared to the lyophilized crude root extract. The Bidens extract formulations were able to inhibit up to 71% of the growth of the parasite in the lowest tested dose, being about five times more active than the crude extract, thus showing significant partial antiplasmodial activity. The dried preparations did not show signals of toxicity in both the in vitro and in vivo assays. The results showed strong evidence that the co-spray drying of B. pilosa root extract with the selected pharmaceutical excipients might stabilize the bioactive compounds and enhance its antimalarial activity compared with the lyophilized crude extract.