Abstract
Parenteral therapy for severe and complicated malaria is necessary, but currently available parenteral antimalarials have their own drawbacks. As for recommended artemisinin-based combination therapy, antimalarial artemether and lumefantrine are limited in parenteral delivery due to their poor water solubility. Herein, the aim of this study was to develop the lipid-based emulsions for intravenous co-delivery of artemether and lumefantrine. The lipid emulsion was prepared by high-speed shear and high-pressure homogenization, and the formulations were optimized mainly by monitoring particle size distribution under autoclaved conditions. The final optimal formulation was with uniform particle size distribution (~ 220 nm), high encapsulation efficiency (~ 99%), good physiochemical stability, and acceptable hemolysis potential. The pharmacokinetic study in rats showed that Cmax of artemether and lumefantrine for the optimized lipid emulsions were significantly increased than the injectable solution, which was critical for rapid antimalarial activity. Furthermore, the AUC0-t of artemether and lumefantrine in the lipid emulsion group were 5.01- and 1.39-fold of those from the solution, respectively, suggesting enhanced bioavailability...Continue Reading
References
Aug 1, 1995·Experimental Parasitology·M KrugliakH Ginsburg
Dec 1, 1995·International Journal for Parasitology·E DeharoH Ginsburg
May 14, 1999·Pharmaceutical Science & Technology Today·A G Floyd
Sep 25, 1999·Clinical Pharmacokinetics·N J WhiteF Ezzet
Sep 5, 2006·Pharmaceutical Research·David F Driscoll
Sep 9, 2006·Journal of Controlled Release : Official Journal of the Controlled Release Society·Jhi-Joung WangJia-You Fang
May 16, 2007·Journal of Pharmaceutical Sciences·Lingling TianXing Tang
Aug 19, 2007·ChemMedChem·Richard K HaynesMelba F Gomes
Jan 23, 2009·Colloids and Surfaces. B, Biointerfaces·Shaimaa S IbrahimNahed D Mortada
Nov 17, 2009·Advanced Drug Delivery Reviews·Nereide Stela Santos-Magalhães, Vanessa Carla Furtado Mosqueira
Oct 12, 2011·Malaria Journal· WahajuddinGirish K Jain
Mar 27, 2012·Biopharmaceutics & Drug Disposition· WahajuddinGirish Kumar Jain
Apr 5, 2013·Infection·P De NardoA Corpolongo
Apr 24, 2013·International Journal of Pharmaceutics·Wei-Cong MaSheng-Jun Mao
Sep 28, 2013·Mini Reviews in Medicinal Chemistry·Muhammad Tayyab AnsariMunawer Khanum
Nov 7, 2013·Advances in Colloid and Interface Science·N P AdityaE B Souto
May 3, 2014·Drug Delivery·Deepa ParasharR S R Murthy
Jul 2, 2014·Antimicrobial Agents and Chemotherapy·Yufan MaTao Chen
Apr 25, 2015·Malaria Journal·Socrates Litsios
Dec 25, 2015·Journal of Controlled Release : Official Journal of the Controlled Release Society·Karl Hörmann, Andreas Zimmer
Oct 25, 2016·International Journal of Pharmaceutics·Priyanka PrabhuVandana Patravale
Jul 21, 2010·Pharmaceuticals·Qigui Li, Peter Weina
Jun 18, 2017·International Journal of Pharmaceutics·Iman HaidarWilliam N Charman
Nov 12, 2017·Journal of Infection and Chemotherapy : Official Journal of the Japan Society of Chemotherapy·Chihiro HasegawaMikio Kimura
Nov 29, 2017·Journal of Liposome Research·Kashif ShakeelFarhan Jalees Ahmad