Development of artemether-loaded nanostructured lipid carrier (NLC) formulation for topical application

Artemether is thermostable at 90–95°C, so has been stably formulated in well selected nanostructured lipid carriers as an alternative sustained release topical regimen devoid of the drug’s extensive nausea–vomiting effect which majorly account for patient non-compliance aside from some contra-indications. Ex vivo study has shown that ART permeates through human excised skin which is known to mimic permeation in vivo. [Display omitted] NLC topical formulation as an alternative to oral and parenteral (IM) delivery of artemether (ART), a poorly water-soluble drug was designed. A Phospholipon 85G-modified Gelucire 43/01 based NLC formulation containing 75% Transcutol was chosen from DSC studies and loaded with gradient concentration of ART (100–750mg). ART-loaded NLCs were stable (−22 to −40mV), polydispersed (0.4–0.7) with d90 size distribution range of 247–530nm without microparticles up to one month of storage. The encapsulation efficiency (EE%) for ART in the NLC was concentration independent as 250mg of ART loading achieved ∼61%. DSC confirmed molecular dispersion of ART due to low matrix crystallinity (0.028J/g). Ex vivo study showed detectable ART amounts after 20h which gradually increased over 48h achieving ∼26% cumulative amount permeated irrespective of the applied dose. This proves that ART permeates excised human epidermis, where the current formulation served as a reservoir to gradually control drug release over an extended period of time. Full thickness skin study therefore may confirm if this is a positive signal to hope for a topical delivery system of ART.