Iodine from brown algae in human nutrition,with an emphasis on bioaccessibility,bioavailability, chemistry,and effects of processing: A systematic review

Brown algae are becoming increasingly popular as a food source and dietary supplement in Europe and other Western countries. As they are highly rich in iodine, they represent a potential new dietary iodine source. Iodine deficiency has been re-emerging in Europe, and it is important to ensure adequate intake through one's diet. However, macroalgae, and especially brown algae, may contain very high amounts of iodine, and both iodine deficiency and excessive iodine may increase the risk of negative health effects. The iodine content of algae or foods containing algae is currently not regulated in the European Union. The aim of this paper is to review the literature to determine the chemical species of iodine in brown algae, the loss of iodine during processing, and the bioavailability and bioaccessibility of iodine. A systematic search of the literature was performed in April 2021, via the databases Web of Science and PubMed. The review includes studies of iodine in brown macroalgae in relation to bioavailability, bioaccessibility, processing and speciation. A meta-analysis was conducted in relation to the following topics: (i) the correlation between total iodine and iodide (I^–) content in brown algae; (ii) the correlation between the loss of iodine during processing and the I^– content; and (iii) the correlation between bioavailability and the I^– content. The bioavailability of iodine from brown algae was generally high, with in vivo bioavailability ranging from 31% to 90%. The in vitro bioavailability of iodine (2%–28%) was systematically lower than in vivo bioavailability (31%–90%), indicating an inadequate in vitro methodology. Processing may reduce the iodine content of brown algae, and a higher I^– content was positively correlated with increased iodine loss during processing. Although processing strategies may reduce the iodine content of brown algae significantly, the iodine content may still be high after processing. These findings may be used in food safety evaluations of brown algae as well as in the development of macroalgae-containing foods with iodine contents suitable for human consumption. Further research on processing techniques to reduce the iodine content in brown macroalgae are warranted.     

Co-products of beef processing enhance non-haem iron absorption in an in vitro digestion/caco-2 cell model

Beef processing produces high volumes of protein rich, low value, ‘waste’ co-products such as offal. Beef improves uptake of low bioavailable non-haem iron (found in vegetables, fortificants, supplements) and this effect is dubbed the ‘meat-factor’, although the underlying mechanism is not fully understood. Here, we investigate whether bovine co-products (kidney, lung, heart) not previously studied share this enhancing potential. This was determined by coupled in vitro digestion of co-products and subsequent caco-2 cell ferritin formation (an intracellular iron storage protein). In this study we show that bovine co-products significantly increase caco-2 cells’ response to non-haem iron from infant rice cereal. The presence of these co-products, (kidney, lung and heart), increased relative uptake (by 207.13%, 171.21%, 265.28%, respectively), to a greater extent than beef (30.23%). Our findings present a novel function for co-products of beef processing that may have potential as food ingredients to improve non-haem iron bioavailability, thus adding value.     

A Novel Approach for Bisphosphonates: Ionic Liquids and Organic Salts from Zoledronic Acid

Novel ionic liquids and organic salts based on mono- or dianionic zoledronate and protonated superbases, choline and n-alkylmethylimidazolium cations, were prepared and characterized by spectroscopic and thermal analyses. Most of the prepared salts display amorphous structures and very high solubility in water and saline solutions, especially the dianionic salts. Among the zoledronate-based ionic compounds, those containing choline [Ch] and methoxyethylmethylimidazolium [C₃OMIM] cations appear to have significant cytotoxicity against human osteosarcoma cells (MG63) and low toxicity toward healthy skin fibroblast cells. Because osteosarcoma is a bone pathology characterized by an increase in bone turnover rate, the results presented herein may be a promising starting point for the development of new ionic pharmaceutical drugs against osteosarcoma.     

In-vitro and in-vivo comparison of T-OA microemulsions and solid dispersions based on EPDC

The goal of this study was to enhance the absorption of a new water-insoluble antitumor lead compound, T-OA (3β-hydroxyolea-12-en-28-oic acid-3, 5, 6-trimethylpyrazin-2-methyl ester). Early-stage preparation discovery concept (EPDC) was employed in this study. Based on this concept, a microemulsion system was chosen as the method of improving bioavailability. The solubility of T-OA was checked in different oils, surfactants and cosurfactants. Ternary phase diagrams were constructed to evaluate the microemulsion domain. Developed high-performance liquid chromatography method was used to determine drug content. The transparent o/w microemulsion formulation composed of oleic acid (oil), Tween 80 (surfactant), ethanol (co-surfactant) and water enhanced the solubility of T-OA up to 20?mg/mL. It was characterized in terms of appearance, content, viscosity, zeta potential, conductivity, morphology and particle size. The particle size distribution, viscosity, conductivity and zeta potential were found to be 70?nm, 15.57?MPa?s, 44.1?μS?cm^?1 and ?0.174, respectively. Oral bioavailability of T-OA microemulsion and oleic acid solution were checked by using rat model. Contrast to the solid dispersion and proto drug, the area-under-the-curve (AUC) of T-OA microemulsion and oleic acid solution were significantly enhanced. The relative bioavailability of T-OA microemulsion was found to be 5654.7%, which is 57-fold higher than the pure drug. Improved T-OA solubility in microemulsion was found sustained 48?h in dilution study. While the solid dispersion may precipitate under the gastrointestinal circumstance based on dilution results. The in-vivo and in-vitro results indicated that, compare to improve the solubility, it is more important to maintain and prolong the T-OA dissolved status, for improvement of the in-vivo absorption.     

Formulation of solid self-nanoemulsifying drug delivery systems using N-methyl pyrrolidone as cosolvent

Atorvastatin calcium (ATRC) is a poor water soluble drug used for treatment of hypercholesterolemia. This research is aimed to improve solubility and dissolution rate of ATRC by formulating into solid self-nanoemulsifying drug delivery system (S-SNEDDS) using N-methyl pyrrolidone (NMP) as cosolvent. Solubility of ATRC was determined in various vehicles. Ternary phase diagrams were constructed to identify stable nanoemulsion region. SNEDDS formulations were evaluated for robustness to dilution, thermodynamic stability study, % transmittance, self-emulsification time, globule size and transmission electron microscopy. The optimized liquid SNEDDS showed robust to all dilutions exhibiting no signs of phase separation or precipitation for 24?h. Liquid SNEDDS was transformed into S-SNEDDS using different adsorbents. Differential scanning calorimetry and scanning electron microscopy studies unravel the transformation of native crystalline state to amorphous state/solubilized state. In vitro dissolution study of S-SNEDDS was found to be significantly higher in comparison to that from plain drug, irrespective of pH (p?ex vivo permeation studies showed a 4.45-fold improvement in apparent permeability coefficient (P_app) from S-SNEDDS compared to plain drug. In conclusion, S-SNEDDS prepared using NMP as cosolvent provides an effective approach for improved oral delivery of ATRC.     

多肽螯合钙的研究进展

钙作为一种必需营养素,在人体中有着极为重要的作用。现如今,补钙制剂在市场上占有极大的份额,但以无机钙和有机钙为主的第一、第二代补钙制剂仍有较大缺陷,吸收率和生物利用率低,而多肽螯合钙作为第三代具有活性结构的生物钙补钙制剂稳定性好、抗干扰能力强、吸收效果好、生物利用度高,因此越来越受到关注。该文对多肽螯合钙的结合机制、制备方法、吸收途径、生物利用度等方面的研究进行综述,以期对补钙制剂的研究及开发提供新思路。     

类蛋白反应修饰的牡蛎肽锌结合物的生物利用性

通过类蛋白反应(Plastein)修饰制备具有较高锌离子结合能力的牡蛎源肽(EVPPEEH),其锌结合能力为161 mg/g。以缺锌型SD大鼠为试验模型,以牡蛎酶解肽-锌结合物OPZ、类蛋白反应修饰的牡蛎酶解肽-锌结合物LPZ和ZnSO4(ZS)为对照,研究牡蛎源肽(EVPPEEH)与锌的结合物(MZ)在体内的生物利用率和生物利用途径。结果表明:MZ组大鼠血清锌水平,股骨锌储备量及肝脏锌含量和肾脏锌含量均显著高于各对照组。脾脏锌含量MZ组和LPZ组恢复程度相似,均显著高于OPZ组和ZS组。MZ组和各对照组大鼠体重和摄食量均显著增加,效果相似。大鼠小肠转锌蛋白(ZnT1)的表达量MZ组与无机锌组差异不是很明显,而小肽转运蛋白(PepT1)的表达量MZ组最高,相对于ZS组上调了20%,显著高于各对照组,说明大鼠小肠对MZ的吸收利用一部分是通过传统锌离子途径,另一部分是通过小肽途径。MZ有望成为一种新型高效的补锌制剂。     

1-脱氧野尻霉素控释微丸的制备工艺优化及其药动学研究

1-脱氧野尻霉素控释微丸采用挤出滚圆和流化床方法进行制备。首先使用羟丙基甲基纤维素和微晶纤维素等辅料制备分散体、丸芯，再使用羟丙基甲基纳米纤维素邻苯二甲酸酯作为主要包衣材料进行包衣，并装入胶囊。采用SEM观察微丸的微观形态，以及测定其产率、脆碎度、密度、水分含量和粒径分布等物理性质，研究结果显示微丸性质符合中国药典标准规定。在体外释药试验中，溶出介质和放置方式对药物释放无显著影响，释放过程符合Baker-Lonsdale模型。对比研究1-脱氧野尻霉素原料药、分散体微丸和控释微丸在比格犬体内的控释特性，结果表明：与1-脱氧野尻霉素原料药相比，分散体微丸和控释微丸分别使1-脱氧野尻霉素的生物利用度提高了183.37%和243.87%。此外，1-脱氧野尻霉素控释微丸的体内-体外研究的相关性分析可知体外溶出和体内吸收之间呈现良好的线性关系。