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

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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.

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Journal: TechConnect Briefs
Volume: 1, Advanced Materials: TechConnect Briefs 2015
Published: June 14, 2015
Pages: 250 - 252
Industry sector: Advanced Materials & Manufacturing
Topic: Nanoparticle Synthesis & Applications
ISBN: 978-1-4987-4727-1