title: Evaluation of novel lipid based formulation of β-Artemether and Lumefantrine in murine malaria model.
abstract: The present investigation aims at formulating lipid based drug delivery system of β-Artemether and Lumefantrine and comparative pharmacological evaluation with innovator formulation. Commercial modified oil and indigenous natural fatty acids comprised the oily phase in developing lipidic formulation of β-Artemether and Lumefantrine. The developed system was characterized for mean globule size, stability by freeze thaw cycles, and birefringence. Developed formulation and innovator formulation were compared for their in vivo anti-malarial activity at different dose levels in male Swiss mice, infected with lethal ANKA strain of Plasmodium berghei. The percent parasitemia, activity against time and animal survival period were examined. On fourth day of antimalarial studies, at normal and ½ dose levels, formulations revealed zero percent parasitemia while control showed 33.92±6.00% parasitemia. At 1/10 dose level, developed and innovator formulations revealed zero percent parasitemia upto 11th day, however, three mice from innovator formulation demonstrated recrudescence after 12th day. Both the formulations at normal dose and ½ dose levels showed 100% activity and survival whereas at 1/10 dose level, innovator formulation showed, 62.5% survival. The developed lipidic system of β-Artemether and Lumefantrine exhibited excellent antimalarial activity with 100% survival.
authors.affiliation: Department of Pharmaceutical Sciences and Technology, Institute of Chemical Technology, N.P. Marg, Matunga, Mumbai 400019, India.
authors.forename: Sushant
authors.initials: S
authors.lastname: Patil
authors.forename: Shital
authors.initials: S
authors.lastname: Suryavanshi
authors.forename: Sulabha
authors.initials: S
authors.lastname: Pathak
authors.forename: Shobhona
authors.initials: S
authors.lastname: Sharma
authors.forename: Vandana
authors.initials: V
authors.lastname: Patravale
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000008:administration & dosage / Q000737:chemistry*; D000077549:Artemether; D037621:Artemisinins / Q000008:administration & dosage / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical; D004195:Disease Models, Animal; D004983:Ethanolamines / Q000008:administration & dosage / Q000737:chemistry*; D005449:Fluorenes / Q000008:administration & dosage / Q000737:chemistry*; D008055:Lipids / Q000737:chemistry*; D000078102:Lumefantrine; D008288:Malaria / Q000188:drug therapy; D008297:Male; D051379:Mice; D018512:Parasitemia / Q000188:drug therapy; D010962:Plasmodium berghei
chemical_list: D000962:Antimalarials; D037621:Artemisinins; D004983:Ethanolamines; D005449:Fluorenes; D008055:Lipids; D000077549:Artemether; D000078102:Lumefantrine
keywords: Artemether; Lipid; Lumefantrine; Parasitemia; Recrudescence; Survival