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Bile salt induced solubilization of methylene blue: Study on methylene blue fluorescence properties and molecular mechanics calculation

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Journal of Pharmaceutical Analysis 2017年第1期7卷 71-75页

作者： Susithra Selvam Ivy Sarkar Department of Chemistry Vel Tech University Avadi Chennai 600062 Tamilnadu India Department of Chemistry Indian Institute of Technology Madras Chennai 600036 Tamilnadu India

Methylene blue(MB) is a hydrophobic drug molecule, having importance both as a staining reagent and pharmaceutical agent. MB is strongly fluorescent, with an emission peak at 686 nm(λ_(ex)665 nm). In the study,the possibility of MB as an extrinsic fluorophore to study the micellization behavior of bile salts(BSs) was carried out. Since BSs are drug delivery systems, the solubilization of hydrophobic MB drug molecule by BSs was achieved and the nature of association of MB with BS media, namely sodium cholate(Na C) and sodium deoxycholate(Na DC) was evaluated. Change in the photophysical properties of MB is monitored through fluorescence intensity and fluorescence anisotropy at emission peak, 686 nm of MB. Molecular mechanics calculations were carried out to evaluate the MB–BS association. The estimated heat of formation, ΔH_f values are –625.19 kcal/mol for MB–Na C and –757.48 kcal/mol for MB–Na DC. The photophysical study also revealed that MB reports the step-wise aggregation pattern of BSs media, as an extrinsic fluorescence probe.

关键词： Methylene blue Sodium deoxycholate Sodium cholate Absorption Fluorescence spectroscopy Molecular mechanics

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Optimization, characterization and in vitro/vivo evaluation of azilsartan nanocrystals

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Asian Journal of Pharmaceutical Sciences 2017年第4期12卷 344-352页

作者： Jingjing Ma Yinxian Yang Yinghua Sun Jin Sun Shenyang Pharmaceutical University

Azilsartan(AZL), a poorly soluble drug, was considered to be fit for nanocrystals to improve its solubility. Our study intended to prepare AZL nanocrystals by means of bead milling method. Eight stabilizers or their binary combination and the milling time were set to be variable factors to optimize AZL nanosuspension formulation, and six types of freezedrying supports were investigated to reduce the aggregation of particles during the solidification. AZL nanocrystals with or without sodium deoxycholate(NaDC) as combined stabilizer with Poloxamer 188(F68) were prepared owning mean particle sizes of about 300 nm and 460 nm. During the screening processes, the formulation containing NaDC showed a smaller particle size and better stability during lyophilization. The irregular shape and crystal form changing in AZL nanocrystals were discovered by various characterizations. And with physical mixture as reference, nanocrystals showed its improvement about in-vitro dissolution and in-vivo bioavailability. In conclusion, the nanocrystals of AZL could be prepared well in our study. Additionally, our results suggested that NaDC was an appreciated excipient on the nanocrystals platform, which can exhibit the abilities of size-reduction and stabilitymaintaining on freeze-drying.

关键词： Azilsartan Nanocrystals Sodium deoxycholate Freeze drying Dissolution Oral bioavailability

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World Journal of Gastrointestinal Oncology 2014年第7期6卷 225-243页

作者： Anil R Prasad Shilpa Prasad Huy Nguyen Alexaner Facista Cristy Lewis Beryl Zaitlin Harris Bernstein Carol Bernstein Department of Pathology Northwest Medical Center Tucson AZ 85741 United States Department of Pathology College of Medicine University of Arizona Tucson AZ 85724 United States College of Arts and Sciences Boston University Boston MA 2215 United States Department of Cellular and Molecular Medicine College of Medicine University of Arizona Tucson AZ 85724 United States Matrix Solutions Inc. Alberta T2R 0V2 Canada

AIM:To investigate the close parallels between our novel diet-related mouse model of colon cancer and human colon cancer.METHODS:Twenty-two wild-type female mice(ages 6-8 wk)were fed the standard control diet(AIN-93G)and an additional 22 female mice(ages 6-8 wk)were fed the control diet supplemented with 0.2%deoxycho-lic acid[diet+deoxycholic acid(DOC)]for 10 mo.Tu-mors occurred in the colons of mice fed diet+DOC and showed progression to colon cancer[adenocarcinoma(AC)].This progression is through the stages of tubular adenoma(TA),TA with high grade dysplasia or ad-enoma with sessile serrated morphology,intramucosal AC,AC stage T1,and AC stage T2.The mouse tumors were compared to human tumors at the same stages by histopathological analysis.Sections of the small and large intestines of mice and humans were evaluated for glandular architecture,cellular and nuclear morphology including cellular orientation,cellular and nuclear atyp-ia,pleomorphism,mitotic activity,frequency of goblet cells,crypt architecture,ulceration,penetration of crypts through the muscularis mucosa and presence of malignant crypts in the muscularis propria.In addition,preserved colonic tissues from genetically similar male mice,obtained from a prior experiment,were analyzed by immunohistochemistry.The male mice had been fed the control diet or diet+DOC.Four molecular markers were evaluated:8-OH-dG,DNA repair protein ERCC1,autophagy protein beclin-1 and the nuclear location of beta-catenin in the stem cell region of crypts.Also,male mice fed diet+DOC plus 0.007%chlorogenic acid(diet+DOC+CGA)were evaluated for ERCC1,beclin-1 and nuclear location of beta-catenin.RESULTS:Humans with high levels of diet-relatedDOC in their colons are at a substantially increased riskof developing colon cancer.The mice fed diet+DOChad levels of DOC in their colons comparable to that ofhumans on a high fat diet.The 22 mice without addedDOC in their diet had no colonic tumors while 20 ofthe 22 mice(91%)fed diet+DOC developed colonictumors.Furthermore,the tumors in 10

关键词：饮食 deoxycholate 老鼠模型结肠癌组织学 Chlorogenic 酸 8-OH-dG Beclin 1 Beta-catenin

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Microrheology and Release Behaviors of Self-Assembled Steroid Hydrogels

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Journal of Materials Science and Chemical Engineering 2015年第8期3卷 6-15页

作者： W. Liang J. R. Guman-Sepulveda S. He A. Dogariu J. Y. Fang Department of Materials Science and Engineering The College of Optics and Photonics University of Central Florida Orlando USA CREOL The College of Optics and Photonics University of Central Florida Orlando USA

A hydrogel is formed by the self-assembly of sodium deoxycholate (NaDC) in aqueous solution with sodium chloride at pH-7.0. The NaDC hydrogel made of the three-dimensional network of nanofibers shows pH-dependent swelling behaviors. Polystyrene particles with a diameter of 100 nm and doxorubicin hydrochloride (DOX) can be easily loaded into the NaDC hydrogel through swelling. By using the loaded polystyrene particles as a light scattering probe, we study the microrheology of the NaDC hydrogel, showing complex viscoelastic properties. The viscous component dominates at both low and high frequencies, while the elastic component dominates in the intermediate range. The cavity size of the nanofiber network can also be estimated to be ~180 nm. We show that the loaded DOX can be slowly released from the hydrogels into aqueous solution. The release profile of DOX is found to depend on the pH value of the solution.

关键词： Sodium deoxycholate Self-Assembly Hydrogels Microrheology Swelling Release

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Detection of Pathogenic Bacteria <i>Staphylococcus aureus</i>and <i>Salmonella</i>sp. from Raw Milk Samples of Different Cities of Pakistan

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Natural Science 2020年第5期12卷 295-306页

作者： Syeda Asma Bano Munazza Hayat Tayyaba Samreen Mohammad Asif Ume Habiba Bushra Uzair

Food-borne diseases are the main public health problem throughout the world. Milk is important component of human diet including fats, proteins, vitamins and minerals. It is a best source of calcium and phosphorus. Different types of pathogenic bacteria like S. aureus and Salmonella enter in milk and then multiply, after multiplication they become active in causing diseases. These bacteria create serious problems for human health. This study aimed to isolate and identify pathogenic bacteria Staphylococcus aureus and Salmonella from raw milk samples of different cities of Pakistan. Primary screening of raw milk samples was done on the basis of morphological, cultural and biochemical techniques. The final identification was made using 16SrRNA sequence analysis. A total of 200 raw milk samples were collected from different cities of Pakistan. Selective medium xylose lysine deoxycholate agar (XLD) and Mannitol salt agar were used for the identification of Salmonella sp. and S. aureus. Staphylococcus aureus produced yellow colonies with yellow zones on Mannitol salt agar. Staphylococcus aureus exhibited gram-positive character with purple coloration and it was detected as cocci-shaped. Biochemically 91 (45%) samples enhibited Catalase, Coagulase, DNase, Urease, Citrate, fermentation tests positive and indole, oxidase and H2S tests negative with nonmotile character, indicating the presence of Staphylococcus aureus. Salmonella sp. was detected as gram negative rods with pink coloration on gram staining. Biochemically 87 (43%) samples revealed catalase, citrate, H2S and fermentation tests positive while oxidase, DNase, Indole and urease tests negative, indicating the presence of Salmonella sp. in these samples. Of the 200 samples tested, 43% were positive for Salmonella, while 45% samples were contaminated with S. aureus. The 16SrRNA sequence analysis confirmed the results of biochemical and cultural characterization by depicting 99% identity of samples with S. aureus and 98% identity with Salmonella spp. The occurrence

关键词： Raw Milk Staphylococcus aureus Salmonella sp. Mannitol Salt Agar Xylose Lysine deoxycholate

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