Development and characterization of nanoemulsion as carrier for the enhancement of bioavailability of artemether

Abstract

The present study aimed to develop a kinetically stable nanoemulsion of artemether with improved solubility, stability and oral bioavailability. Nanoemulsion was prepared by ultrasonication technique using internal oil phase (consisted of the drug dissolved in coconut oil and span 80) and external phase (comprising tween 80 and ethanol dissolved in water). The formulations were optimized using various parameters like percentage transmittance, refractive index, drug content, viscosity, zeta potential and release rate. Stability studies were conducted for a period of 90 days using stability chambers. In vivo studies of the developed formulations were conducted on Wistar rats and data were analyzed statistically. The nanoemulsion as observed under transmission electron microscope were found to be spherical in shape with an average size of 79.0 nm and a zeta potential of -15 mV which indicated of good electrokinetic stability of nanoemulsion . Nanoemulsion was found to be clear and transparent in appearance with a percentage transmittance of 98.2. Refractive index of 1.32 of the nanoemulsion indicated the isotropic nature of the drug. Release rate of the drug from the nanoemulsion formulation was found to be quite significant (P < 0.001) as compared to the plain drug. In vivo oral bioavailability of the nanoemulsion formulation was found to be 2.6-fold higher than the plain drug (˜ 40%) as observed from pharmacokinetic studies. Thus it was observed that nanoemulsion proved itself as a promising alternate for improving the bioavailability of artemether.

Mechanisms of artemether toxicity on single cardiomyocytes and protective effect of nanoencapsulation

“…In an experimental model, artemether induced high mortality (50%) and electrocardiographic disorders in mice surviving the parasitaemia (Souza et al, 2018). To circumvent this problem, artemether nanocarriers have been developed, including lipid nanoparticles (Aditya, Patankar, Madhusudhan, Murthy, & Souto, 2010), liposomes (Chimanuka, Gabriëls, Detaevernier, & Plaizier-Vercammen, 2002), nanocrystals (Shah et al, 2016), and nanoemulsions (Laxmi, Bhardwaj, Mehta, & Mehta, 2015). Oral drug delivery is a convenient administration route for patients (Attili-Qadri et al, 2013).…”

Enhanced acyclovir delivery using w/o type microemulsion: preclinical assessment of antiviral activity using murine model of zosteriform cutaneous HSV-1 infection

“…The transmission electron micrograph revealed spherical nature of the microemulsion droplets (Figure 2(A)). The mean diameter of the optimized formulation was found to be 198.2 nm with polydispersity index of 0.180 (Figure 2(B)) [34,35]. The zeta potential of the prepared microemulsion was found to be 0.279 mV.…”

Engineering of microcomplex of artemether and lumefantrine for effective drug treatment in malaria

“…The release profile of the formulation F4 was found to be better compared to the pure drug samples. The in-vitro drug release profile showed the microcomplex formulation to be a good candidate for effective treatment (Laxmi et al 2014). The drugs artemether and lumefantrine are declared as class 4/3 according to the BCS system by WHO.…”