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71.
A multiple-unit-type oral floating dosage form (FDF) of 5-fluorouracil (5-FU) was developed to prolong gastric residence time,
target stomach cancer, and increase drug bioavailability. The floating bead formulations were prepared by dispersing 5-FU
together with calcium carbonate into a mixture of sodium alginate and hydroxypropyl methylcellulose solution and then dripping
the dispersion into an acidified solution of calcium chloride. Calcium alginate beads were formed, as alginate undergoes ionotropic
gelation by calcium ions and carbon dioxide develops from the reaction of carbonate salts with acid. The evolving gas permeated
through the alginate matrix, leaving gas bubbles or pores, which provided the beads buoyancy. The prepared beads were evaluated
for percent drug loading, drug entrapment efficiency, image, surface topography, buoyancy, and in vitro release. The formulations
were optimized for different weight ratios of gas-forming agent and sodium alginate. The beads containing higher amounts of
calcium carbonate demonstrated instantaneous, complete, and excellent floating ability over a period of 24 hours. The optimized
formulation was subjected to in vivo antitumor studies to check the therapeutic efficacy of the floating dosage forms containing
5-FU against benzo(a)pyrene-induced stomach tumors in albino female mice (Balb/C strain). The multiple-bead FDF was found
to reduce the tumor incidence in mice by 74%, while the conventional tablet dosage form reduced this incidence by only 25%.
Results indicate that FDF performed significantly better than the simple tablet dosage form.
Published: June 22, 2007 相似文献
72.
Paul Prajita Patel Paritosh Verma Suresh K. Mishra Pragyan Sahu Bikash R. Panda Pritam Kumar Kushwaha Gajraj Singh Senapati Shantibhusan Misra Namrata Suar Mrutyunjay 《Cell biology and toxicology》2022,38(1):111-127
Cell Biology and Toxicology - The key to bacterial virulence relies on an exquisite balance of signals between microbe and hosts. Bacterial toxin–antitoxin (TA) system is known to play a... 相似文献
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False smut is a disease of rice inflorescence. The existing systems of disease severity assessment for rice false smut disease are not very sensitive as the ball quality and also the impact of false smut on filled grain number and grain‐filling were not under consideration. Here, a precise assessment method to evaluate the severity of the disease was developed. The ‘yield representative’ (YR) based on ‘mean floret wt.’ and ‘filled grain %’ was simulated for the precise disease severity assessment of rice false smut disease. The single floret weight envisages major yield components irrespective of the type of panicle. Correlation between YR and major yield attributes was studied, and it was observed that YR had significant correlation with ‘filled grain %’ (0.77–0.95) and ‘single spikelet weight’ (0.88–0.98). Significant negative correlation of YR was observed with the chaff percentage, false smut ball number and ball weight. This YR‐based methodology was utilized to assess the disease severity in nine rice cultivars. The disease severity in those nine cultivars was evaluated by the already existing methodologies also. The disease severity measured by the present technique was compared with the disease severity assessed by the old methodologies. The procedure adapted here for disease severity measurement was found to be more informative and useful. It was observed that in case of mild infection, the false smut was enhancing yield attributes. The high‐yielding rice varieties Savitri and Gayatri were found to be tolerant to false smut and may be used as resistant donors. 相似文献
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Amresh Kumar Nidhi N. Prasad Subodh Kumar Sinha 《Physiology and Molecular Biology of Plants》2015,21(1):159-162
Eleven germplasms of faba bean seeds from four agroclimatic regions of Bihar, India, have been investigated to estimate their nutritional (soluble protein, free amino acids, starch, reducing and non reducing sugar, total soluble sugar) and antinutritional (total extractable phenol and condensed tannin/proanthocyanidin) parameters. These parameters were found in varying concentration in all genotypes studied. The highest concentration of total extractable phenol and proanthocyanidin (condensed tannin) (2.56 and 1.59 % leucocyanidin equivalents respectively on dry matter basis) were found in Samastipur while the lowest from Patna (0.95 and 0.426 % leucocyanidin equivalent on dry matter basis). The different nutritional parameters were also found to be in variable concentration among different germplasms viz. total soluble protein ≈ 20–32 %, free amino acids ≈ 188–348 mg/100 g, starch ≈ 27–33 %, reducing sugars ≈ 85–188 mg/100 g, non reducing sugars ≈ 0.7–1.7 % and total soluble sugars ≈ 0.8–1.9 %. 相似文献
79.
David J. Aceti Craig A. Bingman Russell L. Wrobel Ronnie O. Frederick Shin-ichi Makino Karl W. Nichols Sarata C. Sahu Lai F. Bergeman Paul G. Blommel Claudia C. Cornilescu Katarzyna A. Gromek Kory D. Seder Soyoon Hwang John G. Primm Grzegorz Sabat Frank C. Vojtik Brian F. Volkman Zsolt Zolnai George N. Phillips Jr. John L. Markley Brian G. Fox 《Journal of structural and functional genomics》2015,16(2):67-80
80.
Qianzheng Zhu Nidhi Sharma Jinshan He Gulzar Wani Altaf A Wani 《Cell cycle (Georgetown, Tex.)》2015,14(9):1413-1425
During DNA damage response (DDR), histone ubiquitination by RNF168 is a critical event, which orchestrates the recruitment of downstream DDR factors, e.g. BRCA1 and 53BP1. Here, we report USP7 deubiquitinase regulates the stability of RNF168. We showed that USP7 disruption impairs H2A and ultraviolet radiation (UVR)-induced γH2AX monoubiquitination, and decreases the levels of pBmi1, Bmi1, RNF168 and BRCA1. The effect of USP7 disruption was recapitulated by siRNA-mediated USP7 depletion. The USP7 disruption also compromises the formation of UVR-induced foci (UVRIF) and ionizing radiation-induced foci (IRIF) of monoubiquitinated H2A (uH2A) and polyubiquitinated H2AX/A, and subsequently affects UVRIF and IRIF of BRCA1 as well as the IRIF of 53BP1. USP7 was shown to physically bind RNF168 in vitro and in vivo. Overexpression of wild-type USP7, but not its interaction-defective mutant, prevents UVR-induced RNF168 degradation. The USP7 mutant is unable to cleave Ub-conjugates of RNF168 in vivo. Importantly, ectopic expression of RNF168, or both RNF8 and RNF168 together in USP7-disrupted cells, significantly rescue the formation of UVRIF and IRIF of polyubiquitinated H2A and BRCA1. Taken together, these findings reveal an important role of USP7 in regulating ubiquitin-dependent signaling via stabilization of RNF168. 相似文献