Abstract
Artemether and lumefantrine are World Health Organization (WHO) approved combinational therapy for antimalarial action, which exhibits low aqueous solubility and poor oral bioavailability. The present work intended to perform the comparative antimalarial and pharmacokinetic studies for newly designed combinational formulations using carriers such as dry suspension containing nanosponges (ADS) and microneedles (AMN). The nanosponges required for formulation ADS were prepared using the solvent evaporation method, whereas AMN by solvent casting method. The antimalarial test (percentage inhibition test) revealed that formulations showed significant activity towards chloroquine-resistant strain (RKL-9) in comparison to sensitive strain (MRC-2). Rane's test showed that formulations ADS and AMN increased the mean survival time of mice in contrast with the untreated groups. The pharmacokinetic study revealed that the formulation ADS demonstrated similar kinetic profile with increased mean residence time (MRT) of actives, in comparison with marketed preparation (Riamet). However, formulation AMN showed lesser Cmax and AUC but increased MRT, which demonstrated the prolonged presence of actives in the systemic circulation. Thus, the results of antimalarial and pharmacokinetic studies revealed the excellent action of formulations ADS and AMN towards resistant strains and tremendous potential of formulation ADS in escalating the oral bioavailability of actives with improved efficacy, respectively.
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