Development of artemether and lumefantrine co-loaded nanostructured lipid carriers: physicochemical characterization and in vivo antimalarial activity.
BACKGROUND
Artemether and lumefantrine combination therapy is well-accepted for uncomplicated malaria treatment. However, the current available formulation has several pharmacokinetic mismatches such as drug degradation in gastrointestinal tract, erratic absorption, etc. Hence, need of the hour is the injectable formulation, which can overcome the pharmacokinetic mismatch associated with current available formulation in the market.


OBJECTIVE
To fabricate artemether and lumefantrine co-loaded injectable nanostructured lipid carriers (NLCs) formulation.


METHODS
Artemether and lumefantrine co-loaded NLCs were fabricated using homogenization followed by ultra-sonication method. Fabricated NLCs were evalauated for their physicochemical characteristics, and suitability of the formulation for malaria treatment was evaluated using in vivo animal model (Plasmodium berghei-infected mice). Results, discussion and conclusion: Artemether and lumefantrine co-loaded NLCs had a hydrodynamic diameter of ∼ 145 nm with the surface charge of -66 mV. Due to the lipophilic nature of both antimalarial drugs, both single drugs-loaded and co-loaded NLCs have shown high encapsulation efficiency, which is 84% for artemether and 79% for lumefantrine. In vitro drug release study has shown a biphasic drug release pattern, which has shown 63% artemether release and 45% of lumefantrine release over a time period of 30 h. Plasmodium berghei-infected mice treated with artemether and lumefantrine co-loaded NLCs showed better antimalarial activity with respect to parasitemia progression and survivability period.
a ISF College of Pharmacy , Moga , India.
Deepa
D
Parashar
a ISF College of Pharmacy , Moga , India.
N P
NP
Aditya
a ISF College of Pharmacy , Moga , India.
R S R
RS
Murthy
D000818:Animals; D000962:Antimalarials / Q000008:administration & dosage* / Q000494:pharmacology*; D000077549:Artemether; D037621:Artemisinins / Q000008:administration & dosage* / Q000494:pharmacology*; D004337:Drug Carriers; D004983:Ethanolamines / Q000008:administration & dosage* / Q000494:pharmacology*; D005449:Fluorenes / Q000008:administration & dosage* / Q000494:pharmacology*; D008055:Lipids / Q000737:chemistry; D000078102:Lumefantrine; D008288:Malaria / Q000188:drug therapy / Q000469:parasitology; D051379:Mice; D049329:Nanostructures; D010316:Particle Size; D010962:Plasmodium berghei
D000962:Antimalarials; D037621:Artemisinins; D004337:Drug Carriers; D004983:Ethanolamines; D005449:Fluorenes; D008055:Lipids; D000077549:Artemether; D000078102:Lumefantrine
Combination therapy; P. berghei; intraperitoneal; lipid nanoparticles; parasitemia