Novel strategy for encapsulation and targeted delivery of poorly water-soluble active substances

Carriers for targeted delivery and controlled release of poorly water-soluble active substances (PWSAS) are facing three challenges: (a) the encapsulation issues, (b) limitations of PWSAS water solubility, and (c) burst drug release which can be pharmacologically dangerous and economically inefficient. The present study brings a novel strategy for encapsulation and controlled release of PWSAS—caffeine in concentrations which are higher than its maximal water solubility without the possibility of burst effect. The modification of hydrophilic carrier based on poly(methacylic acid) was done using casein and liposomes. To further increase the maximal caffeine loading inside the carrier nicotinamide was used. The release study of the encapsulated PWSAS was elaborated with respect to morphology of the carriers and interactions that could be established between its structural components. The carriers swelling and the release of caffeine and nicotinamide were also investigated depending on caffeine concentration, the presence of different liposomal formulations and the volume ratio of liposomal formulation, in three media with different pH simulating the path of the carrier through the human gastrointestinal tract. The synthesized carriers are promising candidates for encapsulation of PWSAS in concentrations which are higher than its maximal water solubility and for the targeted delivery of those dosages.     

烟酰胺和3-氰基吡啶的HPLC检测

采用高效液相色谱法测定烟酰胺和3-氰基吡啶的含量.色谱条件为:STR-ODSⅡ柱(4.6 mm×150 mm),流动相为甲醇∶水=1 ∶ 3,流速1.000 mL·min-1,检测波长254 nm,柱温30℃.该方法的烟酰胺和3-氰基吡啶检测范围均为1.0～40.0 mg·L-1,烟酰胺的检测限为0.25 mg·L-1...     

Growth of microalgae using CO2 enriched air for biodiesel production in supercritical CO2

The optimum conditions for lipids productivity and CO₂ fixation of two freshwater strains, namely Chlorella sp. and Pseudochlorococcum sp. and a marine strain; namely Nannochlorpsis sp. have been determined in this work. The species were grown autotrophically under aeration with different CO₂ concentrations, ranging from 0.04 to 2% (v/v). The growth was tested in nitrogen sufficient and deficient media at different salinities (0.49–680 mM) and temperatures of 27 and 31 °C. The optimum CO₂ enrichment was found to be 1% (v/v) in both media. Nitrogen starvation resulted in an increase in lipid contents, but at lower growth rate, which resulted in a lower overall lipid productivity. The experimental data were used to determine the kinetic parameters of Haldane model. The Chlorella sp. grew well at salinity levels of up to 460 mM. The highest CO₂ biofixation rate was observed when Chlorella sp. was grown at 27 °C in seawater (230 mM NaCl).Lipids were extracted from harvested marine strain, Nannochlorpsis sp., and enzymatically transesterified to produce biodiesel in supercritical CO₂ (SC–CO₂) medium. It was found that the conversion of biodiesel produced from microalgae lipids was 35% higher than that achieved using lamb fat in a similar system.     

Validation of a Gas Chromatography-Mass Spectrometry Method for the Measurement of the Redox State Metabolic Ratios Lactate/Pyruvate and β-Hydroxybutyrate/Acetoacetate in Biological Samples

The metabolic ratios lactate/pyruvate and β-hydroxybutyrate/acetoacetate are considered valuable tools to evaluate the in vivo redox cellular state by estimating the free NAD+/NADH in cytoplasm and mitochondria, respectively. The aim of the current study was to validate a gas-chromatography mass spectrometry method for simultaneous determination of the four metabolites in plasma and liver tissue. The procedure included an o-phenylenediamine microwave-assisted derivatization, followed by liquid-liquid extraction with ethyl acetate and silylation with bis(trimethylsilyl)trifluoroacetamide:trimethylchlorosilane 99:1. The calibration curves presented acceptable linearity, with a limit of quantification of 0.001 mM for pyruvate, β-hydroxybutyrate and acetoacetate and of 0.01 mM for lactate. The intra-day and inter-day accuracy and precision were within the European Medicines Agency’s Guideline specifications. No significant differences were observed in the slope coefficient of three-point standard metabolite-spiked curves in plasma or liver and water, and acceptable recoveries were obtained in the metabolite-spiked samples. Applicability of the method was tested in precision-cut liver rat slices and also in HepG2 cells incubated under different experimental conditions challenging the redox state. In conclusion, the validated method presented good sensitivity, specificity and reproducibility in the quantification of lactate/pyruvate and β-hydroxybutyrate/acetate metabolites and may be useful in the evaluation of in vivo redox states.     

烟酰胺配合物的合成及晶体形态的电镜观察

为了进一步了解烟酰胺配体的配位特征和结构特点，对配合物Mn(Nica)2Cl2,Fe(Nica)2Cl2,Co(Nica)2Cl2,Ni(Nica)2Cl2,Cu(Nica)2Cl2和Zn(Nica)2Cl2进行了合成和红外光谱、透射电镜、扫描电镜的表征，烟酰胺以吡啶氮与金属离子配位，Mn(Ⅱ），Fe(Ⅱ),Co(Ⅱ)，Ni(Ⅱ）配合物为六方晶体结构，Cu(Ⅱ）配合物为金刚石立方晶体结构。     

Antimicrobial activity of Elettaria cardamomum: Toxicity,biochemical and histological studies

Elettaria cardamomum is one of the most broadly used spices in Moroccan gastronomy. Its antimicrobial activity against both Gram-positive and Gram-negative bacterial species was demonstrated. Likewise, its toxicity was investigated on Swiss albinos mice. Daily, mice were treated orally with 0.003 and 0.3 mg during 7 days. Plasmatic markers and antioxidant defence systems were assessed and histological alterations were evaluated. A significant increase in creatine phosphokinase level was observed. The microscopic evaluation shows that E. cardamomum induce morphological perturbation in mice’s heart. The results show also an inhibitory effect of glyceraldehyde 3-phosphate dehydrogenase and an important increase in the level of thiobarbituric acid reactive substances, succinate dehydrogenase and catalase activities. Results show that E. cardamomum induces toxicity at 0.3 mg/g mouse and affect energy metabolism and oxidative stress.     

Identification of phenolic compounds isolated from pigmented rices and their aldose reductase inhibitory activities

Two anthocyanins (cyanidin-3-O-β-glucoside and peonidin-3-O-β-glucoside) and other phenolic (ferulic acid) were, respectively isolated from black and pigmented brown rices (Oryza sativa L. japonica) and their complete structures were determined by spectroscopic analyses (H NMR, C NMR and MALDI MASS). The HPLC profile of anthocyanins extracted from black rice showed cyanidin-3-O-β-glucoside as the first peak (85%) and peonidin 3-O-β-d-glucoside as the second (15%), while that of pigmented brown rice showed ferulic acid as the first peak (85.7%) and tocols as the second (14.3%). Several tocols were isolated and identified from the unsaponifiable fractions of both rices having some difference on their structures and amounts. The aldose reductase inhibitory activity of isolated compounds was in the following decreasing order: cyanidin-3-glucoside > quercetin > ferulic acid > peonidin-3-glucoside > tocopherol.     

Nicotinamide Mononucleotide Protects against Retinal Dysfunction in a Murine Model of Carotid Artery Occlusion

Cardiovascular abnormality-mediated retinal ischemia causes severe visual impairment. Retinal ischemia is involved in enormous pathological processes including oxidative stress, reactive gliosis, and retinal functional deficits. Thus, maintaining retinal function by modulating those pathological processes may prevent or protect against vision loss. Over the decades, nicotinamide mononucleotide (NMN), a crucial nicotinamide adenine dinucleotide (NAD⁺) intermediate, has been nominated as a promising therapeutic target in retinal diseases. Nonetheless, a protective effect of NMN has not been examined in cardiovascular diseases-induced retinal ischemia. In our study, we aimed to investigate its promising effect of NMN in the ischemic retina of a murine model of carotid artery occlusion. After surgical unilateral common carotid artery occlusion (UCCAO) in adult male C57BL/6 mice, NMN (500 mg/kg/day) was intraperitoneally injected to mice every day until the end of experiments. Electroretinography and biomolecular assays were utilized to measure ocular functional and further molecular alterations in the retina. We found that UCCAO-induced retinal dysfunction was suppressed, pathological gliosis was reduced, retinal NAD⁺ levels were preserved, and the expression of an antioxidant molecule (nuclear factor erythroid-2-related factor 2; Nrf2) was upregulated by consecutive administration of NMN. Our present outcomes first suggest a promising NMN therapy for the suppression of cardiovascular diseases-mediated retinal ischemic dysfunction.