SN-38
<p>One-step mechanochemical preparation and prominent antitumor activity of SN-38 self-micelle solid dispersion</p>
... of SN-38 with disodium glycyrrhizin (Na 2 GA) was prepared by mechanical ball milling (Na 2 ...and SN-38 (Na 2 GA/SN-38-UM), a pure drug SN-38, was prepared for ...
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Characterization of DNA topoisomerase I in three SN-38 resistant human colon cancer cell lines reveals a new pair of resistance-associated mutations
... Top1-DNA cleavage complexes (DPCs) were detected using alkaline elution as previously described [42]. In brief, cells seeded in flasks were radiolabeled overnight with 0.02 μCi/ml [ 14 C]thymidine and chased with ...
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The oncogenic receptor ErbB2 modulates gemcitabine and irinotecan/SN-38 chemoresistance of human pancreatic cancer cells via hCNT1 transporter and multidrug-resistance associated protein MRP-2
... as an indicator of normal biological processes, pathogenic processes, or a pharmacological response to a therapeutic intervention (http://www.biomarkersconsortium.org)” [36]. However, despite the discovery of thousands ...
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Tumour regression and improved gastrointestinal tolerability from controlled release of SN 38 from novel polyoxazoline modified dendrimers
... into SN-38 in the intestines, and enzymatic cleavage of the metabolite SN-38G (SN-38 glucuronide) back into SN-38 during enterohepatic circulation and reabsorption of the ...
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Genetic predisposition to the metabolism of irinotecan (CPT 11) Role of uridine diphosphate glucuronosyltransferase isoform 1A1 in the glucuronidation of its active metabolite (SN 38) in human liver microsomes
... metabolite, SN-38, is glucuronidated by hepatic uridine diphosphate glucuronosyltransferases ...of SN-38, the extent of which is determined by SN-38 ...in SN-38 ...
9
Pharmacokinetics and safety of DTS-108, a human oligopeptide bound to SN-38 with an esterase-sensitive cross-linker in patients with advanced malignancies: a Phase I study
... Vomiting and diarrhea were observed in several patients in this study including two cases of grade 3 vomiting and two cases of grade 3 diarrhea (Tables 2 and 3). Cases of grade 3 diarrhea occurred in two patients with ...
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Value of plasma SN-38 levels and DPD activity in irinotecan-based individualized chemotherapy for advanced colorectal cancer with heterozygous type UGT1A1*6 or UGT1A1*28
... SN-38 and internal standard were dissolved in 50% methanol at a concentration of 1.0 mg/mL and stored at –80°C. To draw a calibration curve, an appropriate volume of standard working solution was added to ...
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STA-8666, a novel HSP90 inhibitor/SN-38 drug conjugate, causes complete tumor regression in preclinical mouse models of pediatric sarcoma
... Heat shock protein 90 (HSP90) is a molecular chaperone that regulates the post-translational folding, stability, and function of many client proteins. A number of these client proteins play critical roles in cancer ...
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In vitro and in vivo evaluation of SN-38 nanocrystals with different particle sizes
... SN-38 (purity 98%) was purchased from Dalian Meilun Biological Technology Co. Ltd. (Dalian, China). Soybean lecithin was obtained from Tywei Pharmaceutical (Shanghai, China). Poloxamer 188 was provided by ...
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The role of intestinal UDP-glucuronosyltransferases in 7-ethyl-10-hydroxy-camptothecin (SN-38) conjugation and toxicity
... MRP2), SN-38 carboxylate biliary clearance was reduced whereas for the lactone form it was unchanged, suggesting a role of mrp2 in the hepatic transport of only the carboxylate (Chu et ...1997). ...
213
DETERMINATION OF SN 38 CONTENTS IN NANOCAPSULES BY CHROMATOGRAPHIC AND SPECTROPHOTOMETRIC METHODS
... Standard stock solutions were prepared at 100µg/mL in acetonitrile. For lactone form, the solutions were diluted with acetonitrile pH adjusted with 0.1 M Hcl (pH 4.5, 100mM) and for carboxylate it was diluted with ...
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Antitumor efficacy of Folic Acid conjugated Polymeric Nanoparticles of SN-38 after oral delivery
... of SN-38 from chitosan nanoparticles in 24 hrs is ...pure SN-38 in PBS, but lesser in simulated colonic ...on SN-38 oral delivery were limited to in vitro cytotoxicity studies ...
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A novel microfluidic liposomal formulation for the delivery of the SN-38 camptothecin: characterization and in vitro assessment of its cytotoxic effect on two tumor cell lines
... by SN-38 on both HeLa and Caco-2 cell lines: a dramatic decrease in cell survival for SN-38-treated cells in relation to control cells was observed, which was that the cytotoxicity of the drug ...
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Transcatheter hepatic therapy with irinotecan eluting beads (DEBIRI) for the treatment of colorectal liver metastases
... agent SN-38 by carboxylesterases 1 & 2 (CES-1 & CES-2 (Guichard et ...1999). SN-38 directly targets the DNA repair enzyme topoisomerase I (Topo-1) promoting apoptotic cell death ...
284
Development and Validation for the Determination of Related Substance in Irinotecan HCL Formulation and its Stability Indicating Studies by RP - HPLC.
... linear in the concentration range of 10.0–2000.0 ng/mL for CPT-11 and 0.5–200.0 ng/mL for 7- ethyl-10-hydroxycamptothecin (SN-38), respectively. The lower limit of quantification (LLOQ) was 10 ng/mL for ...
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Bicarbonate Attenuates Irinotecan Induced Cytotoxicity through Regulation of Both Extracellular and Intracellular pHs in Intestine Cell Line
... of SN-38, the cell was maintained under the same culture conditions for an ad- ditional 4 h period before being loaded with 5 µM Snarf-1 acetoxymethyl acetate for 20 - 40 min at ...
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Human ABC transporter ABCG2/BCRP expression in chemoresistance: basic and clinical perspectives for molecular cancer therapeutics
... Abstract: Adenine triphosphate (ATP)-binding cassette (ABC) transporter proteins, such as ABCB1/P-glycoprotein (P-gp) and ABCG2/breast cancer resistance protein (BCRP), transport various structurally unrelated compounds ...
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sn metrizable spaces and related matters
... Because X is a sequential space, and a regular sequential space with a σ-locally count- able k-network is meta-Lindel¨of (see [10, Proposition 1]), then X has not any σ -locally countable k-network. So X is not an ℵ ...
9
Activity Measurement of Titanium Tin Alloys by Knudsen Effusion Method
... The measurement was carried out for eight compositions for Ti-Sn alloy at 1400 K. The measured effusion rates and the calculated activities are summarized in Table 3. It took 6–9 h in total to measure the effusion ...
5
Reactions in Electrodeposited Cu/Sn and Cu/Ni/Sn Nanoscale Multilayers for Interconnects
... Electron Microscope (FESEM) was used to examine the cross-section of the electrodeposits. The number and size of the voids formed in the Cu/Sn and Cu/Ni/Sn samples were calculated from four micrographs for ...
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