No abstract

The existing armament of drugs for the treatment and prevention of malaria is inadequate due to development of resistance. In addition to this due to lack of economic enticement the rate of new drug development and new drug discovery in the segment of parasitic diseases is very low as compared to the other segments. This has necessitated the better deployment and usage of existing antimalarial drugs as well as discovery of antimalarial activity of drugs which are well characterized for other diseases; these approaches help to reduce the time and cost required for new drug discovery. The present study evaluated the antimalarial activity of antituberculosis drugs rifampicin, isoniazide, and ethambutol in monotherapy and combination in Plasmodium berghei-infected mice. Animals were observed for mortality, parasite progression, and toxicity for a period of 1 month. Rifampicin + isoniazide and rifampicin + isoniazide + ethambutol treatment resulted in an overall survival rate of 60% compared to 0% in vehicle-fed animals by 4 weeks after post-infection without showing any toxicity.

Nanonization is a technology that is often used to enhance aqueous solubility and thus improve bioavailability of poorly soluble molecules. This improvement in bioavailability is due to changes in physicochemical properties such as surface/volume ratio, wettability etc. In this work, material specific coupling and volumetric heating properties of microwaves were utilized to achieve a high degree of supersaturation and nucleation by rapidly and uniformly evaporating the solvent from the binary mixture of solvent and antisolvent. This resulted in the formation of nanosized curcumin nanoparticles suspended in the antisolvent. Nanonization resulted in the formation of curcumin nanoparticles which were ∼160 nm size. The spherical shape of the nanoparticles was visually confirmed by scanning electron microscopy. By applying this approach, we managed to convert large polydispersed curcumin crystals into nanoparticles with considerably decreased crystallinity. This was demonstrated by the decrease in the curcumin's characteristic sharp peaks in the spectral line from 10−30°(2θ) in the XRD studies and reduced enthalpy of melting as observed by DSC studies. As a consequence of this, it potentially increases the apparent solubility, dissolution velocity and oral bioavailability of curcumin. This increases its use in both food and pharmaceutical products. Microwave-assisted nanonization technology has been developed using green solvents like ethanol and water. This should lead to a step change in the development of sustainable nanotechnology for food and pharmaceutical application.