P.O. Nnamani, A.A. Ugwu, E.C. Ibezim, F.C. Kenechukwu, J.D.N. Ogbonna, N.C. Obitte, S.A. Chime, and A.A. Attama
University of Nigeria, Nsukka, Nigeria
pp. 250 - 252
Keywords: malaria, SLN, liquisolid compacts, artemether, lumefantrine
Lumenfantrine-SLN (LUM, 0.2, 0.5, 0.8 and 1%w/w)formulated with Precirol-Transcutol (PT) and Tallow fat-Transcutol (TT) at 3:1 contained surfactants (Poloxamer 188, Polysorbate 80 and Solutol HS). PS, ZP, PDI,morphology, EE, interaction study and in vitro drug release were done. LUM-SLNs were compressed with artemether (ART) to form liquisolid compacts (LUM/ART)evaluated by weight uniformity, hardness, friability, drug content and disintegration time and in-vitro release in biorelevant buffers.Peter’s 4-day curative test was done with CQ-sensitive Plasmodium berghei berghei.Results showed higher yield for PT-SLNs (91.9%) than TT ( 86.2%).Nanoscale particles were obtained with good stability, EE (94.8%)and low enthalpies. Compact properties showed good weight uniformity, thickness, friability, hardness,disintegration time and sustained release in SIF (89%) over SGF (86.6%). Release kinetics showed mixed zero order and Higuchi while non-Fickian diffusion and super case II transport prevailed. Parasitaemia reduction was good (92%) superior to commercial samples (Coartem® 86%) and CQ-phosphate (66%). There was significant difference (p˂0.05) between double strength (4/24 mg/kg) and single strength doses (2/12 mg/kg) of ART/LUM in liquisolid compacts. Therefore alternate-day oral doses of LUM/ART(4/24 mg/kg) can produce 92% parasitaemia reduction to improve patient compliance.