Designing amorphous formulations of polyphenols with naringin by spray-drying for enhanced solubility and permeability

Naringin (NAR), a major flavanone (FVA) glycoside, is a component of food mainly obtained from grapefruit. We used NAR as a food additive to improve the solubility and permeability of hydrophobic polyphenols used as supplements in the food industry. The spray-dried particles (SDPs) of NAR alone show an amorphous state with a glass transition temperature (T_g) at 93.2 °C. SDPs of hydrophobic polyphenols, such as flavone (FVO), quercetin (QCT), naringenin (NRG), and resveratrol (RVT) were prepared by adding varying amounts of NAR. All SDPs of hydrophobic polyphenols with added NAR were in an amorphous state with a single T_g, but SDPs of hydrophobic polyphenols without added NAR showed diffraction peaks derived from each crystal. The SDPs with NAR could keep an amorphous state after storage at a high humidity condition for one month, except for SDPs of RVT/NAR. SDPs with NAR enhanced the solubility of hydrophobic polyphenols, especially NRG solubility, which was enhanced more than 9 times compared to NRG crystal. The enhanced solubility resulted in the increased membrane permeability of NRG. The antioxidant effect of the hydrophobic NRG was also enhanced by the synergetic effect of NAR. The findings demonstrated that NAR could be used as a food additive to enhance the solubility and membrane permeability of hydrophobic polyphenols.     

In vivo evaluation of a mucoadhesive polymeric caplet for intravaginal anti-HIV-1 delivery and development of a molecular mechanistic model for thermochemical characterization

Context and objective: The aim of this study was to develop, characterize and evaluate a mucoadhesive caplet resulting from a polymeric blend (polymeric caplet) for intravaginal anti-HIV-1 delivery.

Materials and methods: Poly(lactic-co-glycolic) acid, ethylcellulose, poly(vinylalcohol), polyacrylic acid and modified polyamide 6, 10 polymers were blended and compressed to a caplet-shaped device, with and without two model drugs 3′-azido-3′-deoxythymidine (AZT) and polystyrene sulfonate (PSS). Thermal analysis, infrared spectroscopy and microscopic analysis were carried out on the caplets employing temperature-modulated DSC (TMDSC), Fourier transform infra-red (FTIR) spectrometer and scanning electron microscope, respectively. In vitro and in vivo drug release analyses as well as the histopathological toxicity studies were carried out on the drug-loaded caplets. Furthermore, molecular mechanics (MM) simulations were carried out on the drug-loaded caplets to corroborate the experimental findings.

Results and discussion: There was a big deviation between the T_g of the polymeric caplet from the T_g's of the constituent polymers indicating a strong interaction between constituent polymers. FTIR spectroscopy confirmed the presence of specific ionic and non-ionic interactions within the caplet. A controlled near zero-order drug release was obtained for AZT (20 d) and PSS (28 d). In vivo results, i.e. the drug concentration in plasma ranged between 0.012–0.332?mg/mL and 0.009–0.256?mg/mL for AZT and PSS over 1–28 d.

Conclusion: The obtained results, which were corroborated by MM simulations, attested that the developed system has the potential for effective delivery of anti-HIV-agents.     

A Potent Mimetic of the Siglec-8 Ligand 6’-Sulfo-Sialyl Lewisx

Siglecs are members of the immunoglobulin gene family containing sialic acid binding N-terminal domains. Among them, Siglec-8 is expressed on various cell types of the immune system such as eosinophils, mast cells and weakly on basophils. Cross-linking of Siglec-8 with monoclonal antibodies triggers apoptosis in eosinophils and inhibits degranulation of mast cells, making Siglec-8 a promising target for the treatment of eosinophil- and mast cell-associated diseases such as asthma. The tetrasaccharide 6’-sulfo-sialyl Lewis^x has been identified as a specific Siglec-8 ligand in glycan array screening. Here, we describe an extended study enlightening the pharmacophores of 6’-sulfo-sialyl Lewis^x and the successful development of a high-affinity mimetic. Retaining the neuraminic acid core, the introduction of a carbocyclic mimetic of the Gal moiety and a sulfonamide substituent in the 9-position gave a 20-fold improved binding affinity. Finally, the residence time, which usually is the Achilles tendon of carbohydrate/lectin interactions, could be improved.     

Synthesis and characterization of poly (linoleic acid)-g-poly(methyl methacrylate) graft copolymer with applying in Au/PLiMMA/n-Si diode

Poly (linoleic acid)-g-poly(methyl methacrylate) (PLiMMA) graft copolymer was synthesized and characterized. PLiMMA graft copolymer was synthesized from polymeric linoleic acid peroxide (PLina) possessing peroxide groups in the main chain by free radical polymerization of methyl methacrylate. Later, PLiMMA was characterized by proton nuclear magnetic resonance (¹H NMR), gel permeation chromatography (GPC), thermal gravimetric analysis (TGA) and differential scanning calorimetry (DSC) techniques. Furthermore, Au/PLiMMA/n-Si diode was fabricated for the purpose of investigating PLiMMA׳s conformity in diodes. The main electrical characteristics of this diode were investigated using experimental current–voltage (I–V) measurements in dark and at room temperature. Obtained results, such as sufficiently high rectifying ratio of 4.5×10⁴, indicate that PLiMMA is a promising organic material for electronic device applications.     

几种酚类抗氧剂在润滑油中的应用

采用旋转氧弹法、高压差示扫描量热法等方法研究了5种酚类抗氧剂对6种润滑油基础油氧化安定性的改善效果。结果表明:向加氢基础油中加入0.25%(质量分数)抗氧剂2246-S和RHY510(含硫酚类抗氧剂),可使HVIWH125,HVIWH150,HVIWH500,KN4006,KN40105种润滑油基础油的诱导期由27～88min提高到226～397min;使HVIWH125,HVIWH150,HVIWH300,HVIWH500,KN4006,KN40106种润滑油基础油的起始氧化温度由193.34～198.90℃提高到205.48～230.27℃。     

Mechanical properties of polyethylene mixtures crystallized under high pressure

The mechanical properties of a medium molecular weight polyethylene (MMW‐PE) and an ultrahigh molecular weight PE (UHMW‐PE) binary mixture with different weight fractions crystallized from the melt at 0.1 and 450 MPa were studied. The tensile modulus, yield stress, and strain were obtained as a function of the weight fractions in the PE mixtures at 25 and 85°C. The tensile modulus in the sample crystallized at 0.1 MPa decreased from 1.5 GPa of pure MMW‐PE to about 0.4 GPa of pure UHMW‐PE with the UHMW‐PE content but it did not decrease with the UHMW‐PE in the sample crystallized at 450 MPa in testing at 25°C. A decreasing rate of the storage modulus E′ of UHMW‐PE in a dynamic measurement for the sample crystallized at 0.1 MPa with the temperature is larger than that of the sample crystallized at 450 MPa. These experimental facts are interpreted in relation to the molecular motion and crystallinity of the sample. © 2003 Wiley Periodicals, Inc. J Appl Polym Sci 87: 1962–1968, 2003     

集中药包与条形药包爆破漏斗及抛掷堆积研究

把集中药包拉成条形药包之后，其爆破漏斗变化有多大?条形药包能否改善抛掷堆积?可否用集中药包的爆破漏斗参数(n、R、R’、P)及经验方法来设计条形药包的爆破漏斗?本试验研究将回答这些问题。     

防止干燥塔塔顶及锥节产生焦粉的方法

描述及分析了干燥塔在生产乳粉过程中出现的塔顶及锥节焦粉现象，并提出了改进方法。     

HP700圆锥破碎机动锥的有限元分析

对HP700圆锥破碎机的主要部件动锥建立了有限元分析模型，用ANSYS软件对动锥进行了有限元强度和刚度分析，结果输出了动锥分布及变形图，对圆锥破碎机的结够设计提供了依据。