Improved antimalarial activity of caprol-based nanostructured lipid carriers encapsulating artemether-lumefantrine for oral administration

Background: Artemether and lumefantrine display low aqueous solubility leading to poor release profile; hence the need for the use of lipid-based systems to improve their oral bioavailability so as to improve their therapeutic efficacy. Aim and objective: The objective of this work was to utilize potentials of nanostructured lipid carriers (NLCs) for improvement of the oral bioavailability of artemether and lumefantrine combination and to evaluate its efficacy in the treatment of malaria. This study reports a method of formulation, characterization and evaluation of the therapeutic efficacies of caprol-based NLC delivery systems with artemether and lumefantrine. Method: The artemether-lumefantrine co-loaded NLCs were prepared using the lipid matrix (5% w/w) (containing beeswax and Phospholipon\uae 90H and Caprol-PGE 860), artemether (0.1%w/w) and lumefantrine (0.6%w/w), sorbitol (4%w/w), Tween\uae 80( 2%w/w as surfactant) and distilled water (q.s to 100%) by high shear homogenization and evaluated for physicochemical performance. The in vivo antimalarial activities of the NLC were tested in chloroquine-sensitive strains of Plasmodium berghei (NK-65) using Peter\ub4s 4-day suppressive protocol in mice and compared with controls. Histopathological studies were also carried out on major organs implicated in malaria. Results: The NLC showed fairly polydispersed nano-sized formulation (z-average:188.6 nm; polydispersity index, PDI=0.462) with no major interaction occurring between the components while the in vivo study showed a gradual but sustained drug release from the NLC compared with that seen with chloroquine sulphate and Coartem\uae. Results of histopathological investigations also revealed more organ damage with the untreated groups than groups treated with the formulations. Conclusion: This study has shown the potential of caprol-based NLCs for significant improvement in oral bioavailability and hence antimalarial activity of poorly soluble artemether and lumefantrine. Importantly, this would improve patient compliance due to decrease in dosing frequency as a sustained release formulation

Amoxicillin loaded-sorbitan monostearate–alginate microparticles as mucoadhesive delivery system for anti-microbial therapy

Antimicrobial resistance has been a challenge to effective antibiotic delivery. Highly technical approaches that meet therapeutic needs are being studied to improve drug bioavailability. This present work seeks to formulate and characterize amoxicillin - loaded sorbitan monostearate-sodium alginate microparticles as mucoadhesive drug delivery for antimicrobial therapy. Three optimized batches of mucoadhesive sorbitan monostearate-alginate microparticles were characterized for particle size, polydispersity index, encapsulation efficiency, viscosity, and mucoadhesivity. Sensitivity test, FTIR spectroscopy and in-vitro drug release were also performed. The particle sizes were between 457 and 872.3 nm. The mean polydispersity index was about 0.569. The encapsulation efficiencies were above 65 %. The pH, viscosity, shear stress and mucoadhesivity were high and decreased gradually with time. The FTIR showed stability and correlation between the formulations and materials used. Sensitivity test showed high susceptibility between 29.00 and 49.33 mm. The drug release followed mostly first order kinetics with R2 > 0.9. Mucoadhesive sorbitan monostearatealginate polymer can be explored as a novel construct for better delivery of amoxicillin.Keywords: sorbitan monostearate, sodium alginate, mucoadhesion, bioavailability, amoxicilli