Design, Optimization, Manufacture and Characterization of Efavirenz-Loaded Flaxseed Oil Nanoemulsions

Abstract

The formation, manufacture and characterization of low energy water-in-oil (w/o) nanoemulsions prepared using cold pressed flaxseed oil containing efavirenz was investigated. Pseudo-ternary phase diagrams were constructed to identify the nanoemulsion region(s). Other potential lipid-based drug delivery phases containing flaxseed oil with 1:1 m/m surfactant mixture of Tween® 80, Span® 20 and different amounts of ethanol were tested to characterize the impact of surfactant mixture on emulsion formation. Flaxseed oil was used as the oil phase as efavirenz exhibited high solubility in the vehicle when compared to other vegetable oils tested. Optimization of surfactant mixtures was undertaken using design of experiments, specifically a D-optimal design with the flaxseed oil content set at 10% m/m. Two solutions from the desired optimization function were produced based on desirability and five nanoemulsion formulations were produced and characterized in terms of in vitro release of efavirenz, physical and chemical stability. Metastable nanoemulsions containing 10% m/m flaxseed oil were successfully manufactured and significant isotropic gel (semisolid) and o/w emulsions were observed during phase behavior studies. Droplet sizes ranged between 156 and 225 nm, zeta potential between −24 and −41 mV and all formulations were found to be monodisperse with polydispersity indices ≤ 0.487.

Fabrication and Evaluation of Quercetin Nanoemulsion: A Delivery System with Improved Bioavailability and Therapeutic Efficacy in Diabetes Mellitus

“…The droplet size of Que-NE was primarily dependent on the linear effect of the Smix ratio (p < 0.001), the interaction effect among Smix and % amplitude (p < 0.05), and the quadratic effect of % amplitude (p < 0.05). Thus, an increased Smix ratio reduced droplet size with a correspondingly higher amplitude due to increased shear and cavitation forces [36]. The other variables that had a significant effect on droplet size were the linear effect of % amplitude (p < 0.05) and the interaction effect between the Smix and sonication time (p < 0.05).…”

“…The T20 and LAB were added to the EO and were titrated against the aqueous phase. The obtained phase diagrams were evaluated in comparison to previous studies, and it was considered that the transparent region obtained in the phase diagrams indicated the nanoemulsion region [36]. Furthermore, the other region exhibiting turbidity was considered conventional emulsion systems.…”

Design, Manufacturing, Characterization and Evaluation of Lipid Nanocapsules to Enhance the Biopharmaceutical Properties of Efavirenz

“…The solubilizing capacity of triglycerides is highly influenced by their intrinsic composition, namely, the degree of unsaturation of their carbon chains. The lower the degree of unsaturation, the higher the solubility [ 26 , 27 , 28 ]. Both Labrafac Lipophile 1349 and MCT oil are made of saturated fatty acids (capric and caprylic fatty acids).…”

Nanoemulsions: The rising star of antiviral therapeutics and nanodelivery system—current status and prospects

“…The self-nano emulsifying oil formulations (SNOFs) of Efz prepared with caproyl 90 and kolliphor EL showed a low percent dissolution efficiency and a high dissolution half-life less than 9 min for Efz under in vitro condition compared to free Efz [ 77 ]. Similarly, low energy water-in-oil NEs of cold-pressed flaxseed oil containing Efz formed using span 20 (28.5%), Tween 80 (28.5%), and ethanol (42.8%) by D-optimised design was found to a stable antiretroviral emulsion [ 78 ].…”