Artemether-loaded nanostructured lipid carrier (NLC) formulation for topical application

摘要: Malaria is caused by parasites of the genus Plasmodium. Malaria due to P. falciparum is the most deadly and predominates in Africa [1]. Globally, an estimated 3.3 billion people were at risk of malaria in 2011, with populations living in sub-Saharan Africa having the highest risk. Malaria is an entirely preventable and treatable disease, provided the currently recommended interventions are properly implemented including vector control through use of insecticide-treated nets (ITNs), indoor residual spraying (IRS), larval control, chemoprevention for the most vulnerable populations, particularly pregnant women and infants, and confirmation of malaria diagnosis through microscopy or rapid diagnostic tests (RDTs) for every suspected case, plus timely treatment with appropriate antimalarial drugs [1, 2]. Antimalarial drug resistance is a major public health problem which hinders the control of malaria. Artemisinin and its derivatives should not be used as monotherapies as poor adherence promotes resistance. Artemether is a potent rapidly-acting schizonticide with oral bioavailability of∼ 45% and available as tablet, capsule and intramuscular (IM) injection. Pharmacokinetics of ART suggests that its clinical efficacy is dependent on formulation [3]. In addition to urgent need for new and effective anti-malarials, there is also crucial need to reformulate existing drugs through the concept of novel DDS to reduce dose-induced side effects, while achieving enhanced aqueous solubility, active targeting of diseased tissues, increased bioavailability and above all, patient-friendly dosage regimens to enhance compliance and reduce resistance due to non …