Pharmacokinetic Characterization of Nano-emulsion Vitamin A, D and E (LaVita) in Rats

Abstract

BACKGROUND:Bioavailability enhancement by solubilization of lipophilic drugs in nano-emulsion has been reported and it may be useful in pharmaceutical and nutraceutical products. This study was performed to compare in vivo bioavailability of nano-emulsion formulation with that of the general product as control. METHODS AND RESULTS:The pharmacokinetics assessment of Vitamin A, D and E complex of nanoemulsion formulation (LaVita), in comparison to the general product, was performed in the male rat plasma by a single oral dose at 20 mL/kg body weight (n=3/group). For nano-emulsion formulation (LaVita), C max of vitamin A and E in plasma were much higher and the area under the curve (AUC) of vitamin A, D and E were 14-63% higher, and the half-life of vitamin E was 2-fold longer than the general product. According to statistical analysis, each C max of vitamin A, D & E was significantly higher (p<0.01, 0.05 and 0.01, respectively) than that of general product. Half-life of vitamin A was significantly higher (p<0.01) and AUC of vitamin A and D were also significantly higher than the general product. CONCLUSION(s): Considering significant increment of C max and AUC, LaVita made of nano-emulsion could be more effective the absorption rate and extent for bioavailability of vitamin A, D & E than those of general product.

Stabilization of Vitamin D in Pea Protein Isolate Nanoemulsions Increases Its Bioefficacy in Rats

“…In the present study, we show that consumption of VitD stably dispersed in a PPI nanoemulsion, created by sonication and pH shifting combined treatment as shown in our previous work [27] resulted Saponaria Molina, as surfactant and showed enhanced micellarization of VitD and absorption in rats [33]. Moreover, after single dose administration of nanoemulsified lipophilic vitamin mixture (i.e., vitamins A, D, E) to rats showed higher plasma area under the curve concentration for these vitamins compared to controls [34]. Though these studies inform on the bioavailability of vitamin D in nanoemulsions, it is important to consider its functionality and efficacy.…”

Stabilization of Vitamin D in Pea Protein Isolate Nanoemulsions Increases Its Bioefficacy in Rats

“…In a recent study, Kadappan et al, (2018) created vitamin D-containing nanoemulsions using Q-NATURALE ® 200 V, an extract from Quillaia Saponaria Molina, as the surfactant and showed enhanced micellarization of VitD and absorption in rats [34]. Moreover, after single dose administration of nanoemulsified lipophilic vitamin mixture (i.e., vitamins A, D, E) to rats showed higher plasma area under the curve concentration for these vitamins compared to controls [35]. Though these studies inform on the bioavailability of vitamin D in nanoemulsions, it is important to consider its functionality and efficacy.…”

Nanoemulsions for food fortification with lipophilic vitamins: Production challenges, stability, and bioavailability

“…Hatanaka et al [112] and Gong et al [114] carried out pharmacokinetic studies using in vivo analyses, and showed that nanoemulsified vitamin E was more bioavailable than its solid capsule forms, which again supports that nanoemulsion delivery systems are good canditates for enhancing bioavailability. Moreover, nanoemulsion delivery systems increased the antioxidant activities of natural vitamin E. The pharmacokinetic study after single dose administration to rat models showed that plasma concentration of the nanoemulsified lipophilic vitamin mixture (vitamins A, D, E) was higher when compared to the general products [113]. To summarize, nanoemulsions exhibit important role in enhancement of the bioavailability of lipophilic compounds with the advantages as below;…”

“…Hatanaka et al and Gong et al carried out pharmacokinetic studies using in vivo analyses, and showed that nanoemulsified vitamin E was more bioavailable than its solid capsule forms, which again supports that nanoemulsion delivery systems are good canditates for enhancing bioavailability. Moreover, nanoemulsion delivery systems increased the antioxidant activities of natural vitamin E. The pharmacokinetic study after single dose administration to rat models showed that plasma concentration of the nanoemulsified lipophilic vitamin mixture (vitamins A, D, E) was higher when compared to the general products . To summarize, nanoemulsions exhibit important role in enhancement of the bioavailability of lipophilic compounds with the advantages as below; The reduced size of nanoemulsion delivery systems promotes increased surface area and provides faster and extensive digestion. Enhanced solubilization rate of the bioactives into mixed micelles during the lipid digestion increases the bioaccessibility. Nanoemulsions facilitate the elimination of first‐pass metabolism and transfer of the chylomicron containing bioactive directly to lymphatic system. Designing nanoemulsion delivery systems with different surfactants/emulsifiers helps to enhance the intestinal permeation. Nanoemulsions may help to increase the residence time of the bioactive lipids within GIT by protecting them from the physicochemical changes and thus improve the absorption of these compounds by enterocyte cells. …”

“…In addition to GIT models, bioactive release studies using dialysis membranes are implemented and caco‐2 cell cultures are also used for in vitro evaluation of the bioavailability . Pharmacokinetic parameters are obtained after in vivo animal and human tests and evaluation of the data were done for investigation of bioavailability of the bioactive lipids . However, in vitro digestion models are more widely used methods than in vivo types due to the ethical, labor‐intensive, and high cost issues of in vivo human or animal models.…”