Background: Nanocrystals have the potential to substantially increase dissolution rate, solubility with subsequent
enhanced bioavailability
via the oral route of a range of poor water soluble drugs. Regardless of other issues, scale up
of the batch size is the main issue associated with bottom up approach.
Material and Methods: Smart nanocrystals of artemisinin (ARM) was produced relatively at large batch sizes (100,
200, 300 and 400ml) compared to our previously reported study by (Shah, et al., 2016). ARM
nanosuspensions/nanocrystals were characterised using zeta sizer, SEM, TEM, DSC, PXRD and RP-HPLC. The
nanosuspensions were finally subjected to
in vitro antimalarial and antimicrobial activity.
Results: The average particle size (PS) for 400 ml batches was 126.5 ±1.02 nm, and the polydispersity index (PI) was
0.194 ± 0.04. The saturation solubility of the ARM nanocrystals was substantially increased to (725.4± 2.0 µg/ml)
compared to the raw ARM in water 177.4± 1.3 µg/ml and stabilizer solution (385.3± 2.0 µg/ml). The IC
50 value of
ARM nanosuspension against
P. vivax was 65 and 21 folds lower than micronized 19.5 ng/mL and unprocessed drug
(6.4 ng/mL) respectively. The ARM nanosuspension was found highly effective compared to unprocessed drug against
all the tested microorganism except
E. coli
,
Shigella
and
C. Albican
.
Conclusion: The simple precipitation-ultrasonication approach was efficiently employed for fabrication of ARM
nanosuspension to scale up the batch size. Similarly, the solubility, antimalarial potential and antimicrobial efficacy of
ARM in the form of nanosuspension were significantly enhanced. Findings from this study can persuade research
interest for further comprehensive studies using animals model.
