Functionalization of cellulose nanocrystals with a potent antimalarial compound: Synthesis, characterization, and biological studies

Cellulosic materials, such as cellulose nanocrystals (CNCs), are biocompatible, biodegradable and have unique and fascinating biomedical applications. Calxinin (CXN), a potent multistage antimalarial compound was functionalised with CNCs to improve biocompatibility and enhance the bioactivity of the resulting CNC-CXN nano-conjugate. Elemental analysis, powder X-ray, SEM, AFM, Infrared, and solid-state NMR spectroscopic techniques confirmed the composition of novel CNC-CXN nano-conjugate. Next, CNC-CXN nano-conjugate did not exhibit apparent cytotoxic effects on the sensitive Vero E6 cell line up to a concentration of 4.66 μg/μl. The CNC-CXN nano-conjugate was also evaluated for its preliminary efficacy on Plasmodium falciparum (3D7) malaria parasite and showed a 50 % inhibitory concentration value of 0.02 μg/μl. Overall, the selectivity index (SI) of the CNC-CXN nano-conjugate significantly improved to 233, indicating its suitability for further validation studies in animal models. [Display omitted] •Biodegradable CNCs were conjugated with Calxinin (CXN) via click chemistry.•CNC-CXN nano-conjugate showed improved thermal stability and structural integrity.•CNC-CXN displayed low cytotoxicity up to 4.66 μg/μl on Vero E6 cells.•High antiplasmodial activity against P. falciparum with a selectivity index of 233.