Dianfa Zhao,Jie Liu,Yunshan Zhou,Lijuan Zhang,Yuxu Zhong,Yang Yang,Baoquan Zhao,Mengru Yang,Yong’an Wang
It is very important to establish a sustained-release pralidoxime chloride (2-PAM) drug system with brain targeting function for the treatment of neurotoxicant poisoning. Herein, Vitamin B1 (VB1), also known as thiamine, which can specifically bind to the thiamine transporter on the surface of the blood–brain barrier, was incorporated onto the surface of MIL-101-NH2(Fe) nanoparticles with a size of ∼100 nm. Pralidoxime chloride was further loaded within the interior of the above resulted composite by soaking, and a resulting composite drug (denoted as 2-PAM@VB1-MIL-101-NH2(Fe)) with a loading capacity of 14.8% (wt) was obtained. The results showed that the drug release rate of the composite drug was increased in PBS solution with the increase of pH (2–7.4) and a maximum drug release rate of 77.5% at pH 4. Experiments on the treatment of poisoning by gavage with the nerve agent sarin in mice combined with atropine revealed that sustained release of 2-PAM from the composite drug was achieved for more than 72 h. Sustained and stable reactivation of poisoned acetylcholinesterase (AChE) was observed with an enzyme reactivation rate of 42.7% in the ocular blood samples at 72 h. By using both zebrafish brain and mouse brain as models, we found that the composite drug could effectively cross the blood–brain barrier and restore the AChE activity in the brain of poisoned mice. The composite drug is expected to be a stable therapeutic drug with brain targeting and prolonged drug release properties for nerve agent intoxication in the middle and late stages of treatment.
Juan Tian,Guilin Peng,Xiaodi Qu,Yunping Yao,Changmo Li
Thiamine (VB 1 ) is an essential water-soluble vitamin that is necessary in our daily diet. However, its instability when exposed to external factors poses a limitation on its application in the food industry. To address this issue and increase its application in fat-rich food systems, this study developed liposoluble VB 1 microcapsules via freeze-drying, utilizing β-cyclodextrin as a wall material and polyglycerol fatty acid ester as an emulsifying agent. The VB 1 microcapsules were characterized in terms of their particle size distribution, morphology, solubility, and stability in soybean oil, as well as their in vitro bioaccessibility. The results showed that the average particle size of VB 1 microcapsules was 83.73 μm with a nonuniform, somewhat wrinkled spherical structure. The solubility of the VB 1 microcapsules in soybean oil was increased to 142.86 mg kg –1 . The retention rates of VB 1 in soybean oil was found to be above 95% after 48 h of UV irradiation and 96.44% after heating for 7 days at 60°C. The presence of VB 1 microcapsules did not significant impact on the oxidation stability of soybean oil. The bioaccessibility of VB 1 in soybean oil was 82.81%. This work provides a useful and novel direction for the application of VB 1 in high-fat diets. Practical applications: VB 1 is one of the B-group vitamins that assists in maintaining normal glucose metabolism. However, it is readily inactivated when exposed to UV radiation, certain pH conditions, and other factors. In this work, the VB 1 microcapsules prepared by freeze-drying exhibited high liposolubility, stability, and bioaccessibility, rendering them suitable for applications in oil-based systems. This work not only provides a new delivery system to facilitate VB 1 supplementation in humans, but also helps to elucidate its application prospect of VB 1 in fat-rich foods, such as edible oil, butter, margarine, rich-fat dressings, and so on, thus improves the application value of VB 1 .
High-efficient separation of molecules is of great significance in food, biotechnology, pharmaceutical and dairy industries. To this end, cationic hyperbranched poly (amido-amine)s (HBPs) with different numbers of quaternary ammonium groups were employed as a new kind of 3D spherical macromonomers to fabricate nanofiltration (NF) membranes, through interfacial polymerization (IP) between cationic HBPs and trimesoyl chloride (TMC) on a polyvinyl chloride ultrafiltration (PVC-UF) hollow fiber membrane surface. Apart from the inner voids inside cationic HBP molecules for fast transport of water molecules, sizes and charge properties of the outer voids between cationic HBP molecules can be modulated by changing the numbers of quaternary ammonium groups on cationic HBP molecule surfaces for enhancing both high permeability and selectivity (water permeance and MgCl 2 rejection rate of the resultant NF membrane are up to 310.5 L m −2 h −1 MPa −1 and 92.0% respectively). Based on the separation mechanism of combined steric and Donnan effects, the resultant NF membrane exhibits ultrahigh retentions to molecules with high molecular weights (MWs) or positive charges, thus molecular-level selectivity to VB12/VB2 (neutral molecules with distinct MWs) or VB1/VB2 (cationic/neutral molecules with similar MWs) can be achieved.
危险品化学品经营许可证（带存储）