Abstract
Artemisinin, the major substance with antimalarial activity of Artemisia annua L., is a poorly water-soluble drug. The development of pellets containing a standardized hydroethanolic extract of A. annua may overcome these drawbacks while offer an intermediate product with good technological properties for subsequent tablet manufacture. This work aimed to obtain and characterize A. annua pellets using the extrusion-spheronization technique. The extract was prepared by percolation and artemisinin content was determined using a validated HPLC method. The standardized extract was then used as a liquid binder in the preparation of pellets with different liquid: solid ratio. The formulation PF5 containing microcrystalline cellulose: A. annua extract (40:58) resulted in pellets with 1.49 ± 0.02 % (w/w) artemisinin, average size of approximately 500 µm and sphericity of 0.82 ± 0.08. These pellets were encapsulated in hard gelatin capsules and the percentage released was higher than 80% in 10 min using 0.1N HCl and phosphate buffer media. These data allow to suggest that the pelletizing strategy used made it possible to achieve the desired artemisinin dissolution and generates perspectives for the potential further use of the A. annua pellets as a solid dosage form for malaria treatment.
Highlights
Artemisia annua L. (Asteraceae) is an herb widely used in traditional medicine to treat malaria with a relatively safe toxicity profile[1,2,3]
The flavonoid content of the leaf powder can vary between 9% and 11% (w/w) and has already been shown to exert antimalarial and antioxidant activity[5] and enhance the activity of artemisinin[6]
Artemisinin is a poorly watersoluble compound with low oral bioavailability[7] when administered alone, its use from A. annua extracts is related to an improvement in bioavailability[2]
Summary
Artemisia annua L. (Asteraceae) is an herb widely used in traditional medicine to treat malaria with a relatively safe toxicity profile[1,2,3]. Artemisinin is a sesquiterpene lactone isolated from the aerial parts of A. annua This compound has an endoperoxide bridge crucial for its potent antimalarial activity at nanomolar concentrations[3,4]. The flavonoid content of the leaf powder can vary between 9% and 11% (w/w) and has already been shown to exert antimalarial and antioxidant activity[5] and enhance the activity of artemisinin[6]. Other phytochemicals in this genus are therapeutically active[2] denoting the relevance of administering the phytotherapeutic complex for treating malaria and other diseases. Artemisinin is a poorly watersoluble compound with low oral bioavailability[7] when administered alone, its use from A. annua extracts is related to an improvement in bioavailability[2]
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