Search Results (3)

The bioavailability of n-3 long-chain polyunsaturated fatty acids (n-3 LCPUFAs) has shown to be greatly influenced by their location in the triacylglycerol backbone. Therefore, the synthesis of structured acylglycerols (SAcyl), which include eicosapentaenoic acids (EPAs) or docosahexaenoic acids (DHAs) at the sn-2 position, has attracted a great interest. The objective of this study was to optimize the synthesis process of a SAcyl from commercial refined salmon oil and an EPA/DHA concentrate in order to enhance the positioning of EPA and DHA in the sn-2 location of the glycerol moiety. For this purpose, immobilized lipase B from Candida antarctica (nonspecific) was used for the acidolysis process under the CO₂ supercritical condition. As a result of carrying out a Draper-Lin composite design through the response surface methodology of 18 experiments, an optimized extraction including SAcyl compounds was obtained. Mass spectrometry (MALDI-TOF) analysis was employed to identify the EPA/DHA location at the sn-2 position in the resulting glycerol moiety. In the fraction obtained, an increase in the EPA and DHA content at the sn-2 position was detected. Remarkably, the optimized SAcyl obtained after 6 h, 82 bar, and 60 °C led to the highest EPA/DHA yield at the sn-2 position in the resulting molecule. Full article

Electromembranes increase the efficiency of metal transport in liquid-phase microextraction systems by applying an electric potential, which accelerates the transport. Nevertheless, to get high extraction percentages in short extraction times it is necessary to take into account a great variety of factors, and multivariate optimization techniques are the best alternative to determine the most influential variables and to optimize the extraction process. In this work, a fractional factorial design was applied to determine the most influential variables in the extraction of silver by electromembranes. Thus, the effect of tri-isobutylphosphine sulphide (Cyanex 471x) concentration in the organic solution, sodium thiosulphate concentration in the acceptor solution, nitrate concentration in the sample solution, extraction time, stirring rate and electric potential on the enrichment factor were studied. Once the most important variables were selected, a small composite design (Draper–Lin) was used to obtain their optimal values to maximize the enrichment factor. Under these conditions, an experimental enrichment factor of 49.91 ± 3.95 was achieved after 22 min. Finally, the effect of saline matrix on the enrichment factor was tested and the optimized system was successfully applied to analyse silver concentrations at ultratrace levels, within the range of 7–29 ng·L⁻¹ in different real seawater samples. Full article

Critical adverse effects and frequent administration, three times per day, limit the use of flutamide (FLT) as a chemotherapeutic agent in the treatment of prostate cancer. Therefore, our research aimed to develop new cholesterol-based nanovesicles for delivering FLT to malignant cells in an endeavor to maximize its therapeutic efficacy and minimize undesired adverse effects. Draper–Lin small composite design was used to optimize the critical quality attributes of FLT-loaded niosomes and ensure the desired product quality. The influence of the selected four independent variables on mean particle size (Y₁), zeta potential (Y₂), drug entrapment efficiency (Y₃), and the cumulative drug release after 24 h (Y₄) was examined. The optimized nanovesicles were assessed for their in vitro cytotoxicity, ex-vivo absorption via freshly excised rabbit intestine as well as in vivo pharmacokinetics on male rats. TEM confirmed nanovescicles’ spherical shape with bilayer structure. Values of dependent variables were 748.6 nm, −48.60 mV, 72.8% and 72.2% for Y₁, Y₂, Y₃ and Y₄, respectively. The optimized FLT-loaded niosomes exerted high cytotoxic efficacy against human prostate cancer cell line (PC-3) with an IC₅₀ value of 0.64 ± 0.04 µg/mL whilst, it was 1.88 ± 0.16 µg/mL for free FLT. Moreover, the IC₅₀ values on breast cancer cell line (MCF-7) were 0.27 ± 0.07 µg/mL and 4.07 ± 0.74 µg/mL for FLT-loaded niosomes and free FLT, respectively. The permeation of the optimized FLT-loaded niosomes through the rabbit intestine showed an enhancement ratio of about 1.5 times that of the free FLT suspension. In vivo pharmacokinetic study displayed an improvement in oral bioavailability of the optimized niosomal formulation with AUC and C_max values of 741.583 ± 33.557 μg/mL × min and 6.950 ± 0.45 μg/mL compared to 364.536 ± 45.215 μg/mL × min and 2.650 ± 0.55 μg/mL for the oral FLT suspension. With these promising findings, we conclude that encapsulation of FLT in cholesterol-loaded nanovesicles enhanced its anticancer activity and oral bioavailability which endorse its use in the management of prostate cancer. Full article