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Abstract
Previous studies reported low benznidazole (BNZ) loading in conventional emulsions due to the weak interaction of the drug with the most common oils used to produce foods or pharmaceuticals. In this study, we focused on how the type of surfactant, surfactant-to-oil ratio w/w (SOR) and oil-to-water ratio w/w (OWR) change the phase behavior of different lipid-based drug delivery systems (LBDDS) produced by emulsion phase inversion. The surfactant mixture composed of soy phosphatidylcholine and sodium oleate (1:7, w/w, hydrophilic lipophilic balance = 16) stabilized medium chain triglyceride in water. Ten formulations with the clear aspect or less turbid dispersions (five with the SOR ranging from 0.5 to 2.5 and five with the OWR from 0.06 to 0.4) were selected from the phase behavior diagram to assess structural features and drug-loading capacity. The rise in the SOR induced the formation of distinct lipid-based drug delivery systems (nanoemulsions and liquid crystal lamellar type) that were identified using rheological measurements and cross-polarized light microscopy images. Clear dispersions of small and narrow droplet-sized liquid-like nanoemulsions, Newtonian flow-type, were produced at SOR from 0.5 to 1.5 and OWR from 0.12 to 0.4, while clear liquid or gel-like liquid crystals were produced at SOR from 1.5 to 2.5. The BNZ loading was improved according to the composition and type of LBDDS produced, suggesting possible drug location among surfactant layers. The cell viability assays proved the biocompatibility for all of the prepared nanoemulsions at SOR less than 1.5 and liquid crystals at SOR less than 2.5, demonstrating their promising features for the oral or parenteral colloidal delivery systems containing benznidazole for Chagas disease treatment.
Highlights
Several research areas have considered the manipulation of matter at the nanoscale due to the flexibility and innumerable opportunities that nanotechnology can offer for different applications
Possible loading of specific targeting molecules, such as cholesterol or folic acid, can improve drug distribution in the tissues affected by cancer and reduce side effects [5]
The use of the same strategy for the treatment of intracellular infections caused by unicellular parasites of the Trypanosoma genus can improve the efficacy of antichagasic drugs
Summary
Several research areas have considered the manipulation of matter at the nanoscale due to the flexibility and innumerable opportunities that nanotechnology can offer for different applications. Lipid-based drug delivery systems (LBDDS), such as nanoemulsions (NE), have been successfully applied in the food, beverage, chemical, cosmetic and pharmaceutical industries due to their ability to load non-polar ingredients in small-sized oil droplet dispersions [1,2]. Interesting characteristics, such as stability, optical translucency and solvent capacity make these LBDDS a unique nanocarrier for poorly water-soluble drugs [3,4]. The use of the same strategy for the treatment of intracellular infections caused by unicellular parasites of the Trypanosoma genus can improve the efficacy of antichagasic drugs. Chagas disease is one of the most important public health problems in Latin America, causing morbidity, long-term disability and mortality [6]
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