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.
Highlights
The human immunodeficiency virus (HIV) is a global health burden
Medium chain triglycerides (MCT) containing oils are best for Lipid-based drug delivery systems (LBDDS) as they are resistant to oxidation and possess high solvent capacity when compared to long-chain triglycerides (LCT) oils because of the high effective concentration of ester functional groups in the oil [41]
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Summary
The human immunodeficiency virus (HIV) is a global health burden. In efforts to improve access to HIV drugs, simplification of process chemistry, reformulation, dose reduction, inclusion of new drug classes and new therapeutic strategies have been developed and contributed to the reduction of the HIV burden [2]. Efavirenz (EFV) is a non-nucleoside reverse-transcriptase inhibitor (NNRTI) used, in combination, for first line treatment of HIV. EFV is a BCS Class II or poorly soluble and highly permeable compound with an aqueous solubility of
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