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Stability of astaxanthin-loaded nanostructured lipid carriers as affected by pH, ionic strength, heat treatment, simulated gastric juice and freeze-thawing.

ABSTRACT: Nanostructured lipid carriers (NLCs) offer many potential benefits for incorporating lipophilic molecules into clear/opaque food systems. In this study, the influence of pH, ionic strength, thermal treatment, simulated gastric juice (SGJ), and freeze-thawing on the stability of astaxanthin-loaded NLCs (Ax-NLCs) was examined. Ax-NLCs (containing ?-tocopherol and ethylenediaminetetraacetic acid as antioxidants) were stabilized with Tween 80 and lecithin (Z-average size: 94 nm), and studied for the above mentioned purpose. The size of Ax-NLCs increased at low pH values (?5), high NaCl concentrations (?50 mM), and slightly at SGJ, mainly because of decreasing the ?-potential. Moreover, thermal treatment at 80/90 °C led to an increase in Ax-NLCs size. Glycerol was found as an appropriate cryoprotectant for preventing aggregation of Ax-NLCs during freeze-thawing. pH, ionic strength, heat and SGJ had no drastic effects on the chemical stability of astaxanthin in NLCs. These results have valuable implications for the utilization of food-grade NLCs.

SUBMITTER: Tamjidi F

PROVIDER: S-EPMC5602976 | biostudies-literature | 2017 Sep

REPOSITORIES: biostudies-literature

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Stability of astaxanthin-loaded nanostructured lipid carriers as affected by pH, ionic strength, heat treatment, simulated gastric juice and freeze-thawing.

Tamjidi Fardin F Shahedi Mohammad M Varshosaz Jaleh J Nasirpour Ali A

Journal of food science and technology 20170719 10

Nanostructured lipid carriers (NLCs) offer many potential benefits for incorporating lipophilic molecules into clear/opaque food systems. In this study, the influence of pH, ionic strength, thermal treatment, simulated gastric juice (SGJ), and freeze-thawing on the stability of astaxanthin-loaded NLCs (Ax-NLCs) was examined. Ax-NLCs (containing α-tocopherol and ethylenediaminetetraacetic acid as antioxidants) were stabilized with Tween 80 and lecithin (Z-average size: 94 nm), and studied for the ...[more]

PMID: 28974798

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Project description:Dendritic cells (DCs) are promising targets for drug delivery, as they can induce immunity or tolerance. The current study aims to examine the potential of using nanostructured lipid carriers (NLC) as delivery systems for human DC by evaluating nanoparticle internalization, cell labeling, and drug activity. NLC were formulated incorporating the fluorochrome fluorescein isothiocyanate (FITC-NLC) or the natural anti-inflammatory molecule resveratrol (rsv-NLC). Primary human DCs were differentiated from peripheral blood monocytes, and the innovative imaging flow cytometry technique was used to examine FITC-NLC internalization. The capacity of rsv-NLC to inhibit DC activation in response to proinflammatory cytokine tumor necrosis factor-α (TNF- α) was investigated by conventional flow cytometry. A combination of imaging and conventional flow cytometry was used to assess NLC cytotoxicity. The results obtained indicate that both NLC formulations were stable over time, with mean diameter <200 nm and highly negative zeta potential (about -30 mV). When DCs were placed in contact with NLC, imaging flow cytometry clearly showed that DCs efficiently internalized FITC-NLC, with nearly 100% of cells internalizing nanoparticles upon 1 hour of incubation. Both immature and mature DCs internalized NLC to high and comparable levels, and without cytotoxicity. Stimulating DC with TNF-α in the presence of rsv-NLC revealed that, using these nanoparticles, very small concentrations of rsv were sufficient to significantly decrease surface expression of activation marker CD83 (5 µM) and major histocompatibility complex-class II molecule human leukocyte antigen - antigen D related (10 µM), both upregulated in response to TNF-α stimulation. Rsv-NLC were compared with free rsv; at 5 µM, rsv-NLC were able to inhibit nuclear factor κ beta phosphorylation and significantly decrease the level of interleukin-12/23, both upregulated in response to TNF-α, while 10 µM free rsv were needed to promote a similar effect. Taken together, the results presented show that NLC are suitable carriers of fluorescent labels or bioactive molecules for human DCs, leading to inflammation modulation.

Project description:Pharmacological treatments of central nervous system diseases are always challenging due to the restrictions imposed by the blood–brain barrier: while some drugs can effectively cross it, many others, some antiepileptic drugs among them, display permeability issues to reach the site of action and exert their pharmacological effects. The development of last-generation therapeutic nanosystems capable of enhancing drug biodistribution has gained ground in the past few years. Lipid-based nanoparticles are promising systems aimed to improve or facilitate the passage of drugs through biological barriers, which have demonstrated their effectiveness in various therapeutic fields, without signs of associated toxicity. In the present work, nanostructured lipid carriers (NLCs) containing the antiepileptic drug phenobarbital were designed and optimized by a quality by design approach (QbD). The optimized formulation was characterized by its entrapment efficiency, particle size, polydispersity index, and Z potential. Thermal properties were analyzed by DSC and TGA, and morphology and crystal properties were analyzed by AFM, TEM, and XRD. Drug localization and possible interactions between the drug and the formulation components were evaluated using FTIR. In vitro release kinetic, cytotoxicity on non-tumoral mouse fibroblasts L929, and in vivo anticonvulsant activity in an animal model of acute seizures were studied as well. The optimized formulation resulted in spherical particles with a mean size of ca. 178 nm and 98.2% of entrapment efficiency, physically stable for more than a month. Results obtained from the physicochemical and in vitro release characterization suggested that the drug was incorporated into the lipid matrix losing its crystalline structure after the synthesis process and was then released following a slower kinetic in comparison with the conventional immediate-release formulation. The NLC was non-toxic against the selected cell line and capable of delivering the drug to the site of action in an adequate amount and time for therapeutic effects, with no appreciable neurotoxicity. Therefore, the developed system represents a promising alternative for the treatment of one of the most prevalent neurological diseases, epilepsy.

Dataset Information

Stability of astaxanthin-loaded nanostructured lipid carriers as affected by pH, ionic strength, heat treatment, simulated gastric juice and freeze-thawing.

Publications

Stability of astaxanthin-loaded nanostructured lipid carriers as affected by pH, ionic strength, heat treatment, simulated gastric juice and freeze-thawing.

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