Advanced Materials: TechConnect Briefs 2015Advanced Materials TechConnect Briefs 2015

Nanoparticle Synthesis & Applications Chapter 5

Sustained-release liquisolid compacts of lumenfantrine-artemether as alternate-dayregimen for malaria treatment to improve patient compliance

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.