Synthesis and bio performance of encapsulated antimalarial co-artemeter in mesoporous nanosilica vesicle

Abstract

Nano carrier vessel is a new approach for ultimate delivery of drugs. This research work synthesised Mobile Composition of Matter (MCM-41) [1] for loading of two antimalarial drugs: MCM-41Artemether(ATM) [2] and MCM-41Lumefantrine(LFT) [3] under varying time, pH and temperature effects. FT-IR spectra depict major functional groups of the silanol group (Si-OH) and silaxone (Si-O) at 3450 and 964 cm^-1, respectively for the 1, while 2 and 3 exhibited only functional groups similar to the parent silica core. 1 had average pore diameter of 5.16 nm while 2 and 3 pore sizes decreased to 4.04 and 3.16 nm, respectively due to the adsorption of the drugs. Morphology of 1 is spherical while 2 and 3 have distorted rod-like shapes attributed to the drugs impregnation as obtained from SEM. The optimal loading conditions of 2 at pH 3.5 ambient temperature, and 3 h gave drug loading capacity (DLC) of 79% and entrapment efficiency (EE) of 65% compared to 3 with DLC of 77% and EE of 50% attributable to the size effect. For the in vitro kinetic release of 2 at 1 h, ambient temperature and pH 3.5 gave 61.4% optimal release, which was very much higher compared to 3 of 7.4% at 0.5 h with other conditions similar. The in vivo measurement of 1 showed better bio performance for Plasmodium berghei NK65 parasite clearance in infected mice on the third day compared to 2 or 3 for nanodrugs and the individual parent drugs. This study confirmed the suitability of 1 for better delivery of ATM and LFT antimalarial drugs.