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Release of anticancer drug 5-Fluorouracil from Different Ionically Crosslinked Alginate Beads

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Journal of Biomaterials and Nanobiotechnology 2012年第4期3卷 469-479页

作者： Merve Olukman Oya Sanli Ebru Kondolot Solak Department of Chemistry Faculty of ScienceGazi UniversityAnkaraTurkey Department of Chemistry and Chemical Processing Technology Ataturk Vocational High SchoolGazi UniversityAnkaraTurkey

In this research;the release of 5-Fluorouracil (5-FU) from different ionically crosslinked alginate (Alg) beads was investigated by using Fe3+, Al3+, Zn2+, and Ca2+, ions as crosslinking agent. The prepared beads were characterized by Fourier Transform Infrared Spectroscopy (FTIR) Differential Scanning Calorimetry (DSC) and Scanning Electron Micros-copy (SEM). The drug release studies were carried out at three pH values 1.2, 6.8 and 7.4 respectively each for two hours. The effects of the preparation conditions as crosslinker type, drug/polymer (w/w) ratio, crosslinker concentration and time of exposure to crosslinker on the release of 5-FU were investigated for 6 hours at 37℃. It was observed that 5-FU release from the beads followed the order of Fe > Zn > Al > Ca-Alg and increased with increasing drug/polymer ratio. At the end of 6 hours, the highest 5-FU release was found to be 90% (w/w) for Fe-Alg beads at the drug/polymer ratio of 1/8 (w/w), crosslinker concentration of 0.05 M, exposure time of 10 minutes respectively. The swelling measurements of the beads supported the release results. Release kinetics was described by Fickian and non-Fickian approaches.

关键词： anticancer drug pH Responsive Release Alginate Ionically Crosslinking Controlled Release 5-Fluorouracil

Comparison of anticancer drug Preparation Techniques between Chemotherapy Specialist Pharmacists and Non-Chemotherapy Pharmacists Using Eye-Tracking Techniques

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Pharmacology & Pharmacy 2023年第8期14卷 229-238页

作者： Yuka Miyachi Yukina Miyagi Saori Gocho Chika Nakayama Masayuki Ejiri Masayuki Takeuchi Masafumi Ohnishi Taeyuki Oshima College of Pharmacy Kinjo Gakuin University Nagoya Japan Graduate School of Medicine Aichi Medical University Nagakute Japan Department of Pharmacy Nagoya Ekisaikai Hospital Nagoya Japan Faculty of Pharmacy Gifu University of Medical Science Kani Japan Department of Pharmacy Aichi Medical University Hospital Nagakute Japan

anticancer drug preparation by pharmacists is a critical task directly related to medical incidents. This study examined the factors influencing medical errors in chemotherapy, that is, errors by specialist pharmacists (CPh) and pharmacists in other departments (NCPh), by measuring their gaze during the preparation of anticancer drugs. The eye-tracking results showed that the gazing time of NCPh was significantly longer than that of CPh for items such as “preparation of a closed-system device” and “preparation of the syringe” and all preparation times (P drugs on a regular basis, indicating their lack of familiarity with the process. There was no significant difference in gaze ratio between CPh and NCPh. This outcome was suggested to be a result of the use of an anticancer drug preparation support system. The results for the pupil diameter variation rate showed that NCPh were significantly more mydriatic in the “mixing injections” category than CPh. However, CPh tended to be more mydriatic in the “checking” category. CPh exhibited a smooth workflow and focused on the important items to be checked. This study showed that the differences in procedure flow and concentration points may lead to errors. Furthermore, the results are of interest from the perspective of medical incident prevention. They will be useful in identifying potential human factors, such as where the pharmacist focuses their attention by measuring eye movements.

关键词： Eye Tracking Medicine Inspection anticancer drug Pharmacists

Hollow-structured nanoparticles as an anticancer drug carrier

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中国药理学与毒理学杂志 2021年第10期35卷 781-781页

作者： ZHU Xiao-ming WU Xuan CHEN Jian-li WAN Hong-ye State Key Laboratory of Quality Research in Chinese Medicine Macao University of Science and TechnologyMacaoChina

Many drug candidates identified from natural products are poorly *** surfactants used to disperse the hydrophobic anticancer drugs in water may cause a serious of acute hypersensitivity *** provides an alternative strategy for delivery of anticancer *** can be encapsulated or attached to the nanomaterials such as lipids,polymers and solid-core *** the present study,porous inorganic nanoparticles have been utilized for delivery of water-insoluble anticancer *** synthesized nanoparticles were functionalized with different organic *** porous nanoparticles were readily internalized by human glioblastoma U-87 MG cells,and didn′t display *** internalized nanoparticles were mainly localized in endosomes/lysosomes in *** the hydrophobic curcumin and carfilzomib as model drugs,intracellular delivery of hydrophobic anticancer drugs by the porous inorganic nanoparticles was *** porous nanoparticle-based encapsulation of hydrophobic drug provides the aqueous dispersion of the *** endosomes/lysosomes mimicking buffers with a pH of 4.5-5.5,pH-dependent drug release was observed from drug loaded *** intracellular drug content and cytotoxicity were significantly higher for drug loaded nanoparticles than free *** results suggested porous inorganic nanoparticles might be a promising intracellular carrier for hydrophobic anticancer drugs.

关键词： hollow nanopoarticles anticancer drug drug delivery curcumin

Investigation of the redox status in H22 hepatocellular carcinoma xenografts treated by a novel anticancer drug-ethaselen

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Journal of Chinese Pharmaceutical Sciences 2009年第3期18卷 245-251页

作者：王立辉曾慧慧北京大学天然药物与仿生药物国家重点实验室北京100191

We investigated the redox status of H22 hepatocellular carcinoma xenografts treated with various doses of ethaselen, a novel anticancer drug targeting thioredoxin reductase （TrxR）. The concentrations of low molecular weight antioxidant g!utathione （GSH） and malondialdehyde （MDA）, a product of lipid peroxidation, as well as the activities of important antioxidant enzymes were measured for elucidating the redox status of H22 tumor tissues. We found that the decreased GSH level, decreased thioredoxin reductase and superoxide dismutase （SOD） activities as well as increased MDA content were closely related to the tumor growth inhibition and ethaselen doses. Glutathione peroxidase （GPx） and glutathinne reductase （GR） activities are also affected by ethaselen treatment. However, the catalase （CAT） activity remains unchanged. Finally, we studied the relationship of tumor growth inhibition caused by ethaselen with these redox factors. This study showed that ethaselen could elevate the oxidative stress to suppress the H22 tumor growth in mice model.

关键词： Ethaselen Thioredoxin reductase inhibitor anticancer drug Redox status Antioxidant system Hepatocellular carcinoma

iGMDR:Integrated Pharmacogenetic Resource Guide to Cancer Therapy and Research

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Genomics, Proteomics & Bioinformatics 2020年第2期18卷 150-160页

作者： Xiang Chen Yi Guo Xin Chen Institute of Pharmaceutical Biotechnology and the First Affiliated Hospital Department of Radiation Oncology Zhejiang University School of MedicineHangzhou 310058China Department of Polymer Science and Engineering and Key Laboratory of Adsorption and Separation Materials and Technologies of Zhejiang Province Zhejiang UniversityHangzhou 310027China Joint Institute for Genetics and Genome Medicine between Zhejiang University and University of Toronto Zhejiang UniversityHangzhou 310058China

Current pharmacogenetic studies have obtained many genetic models that can predict the therapeutic efficacy of anticancer *** some of these models are of crucial importance and have been used in clinical practice,these very valuable models have not been well adopted into cancer research to promote the development of cancer therapies due to the lack of integration and standards for the existing data of the pharmacogenetic *** this purpose,we built a resource investigating genetic model of drug response(iGMDR),which integrates the models from in vitro and in vivo pharmacogenetic studies with different omics data from a variety of technical *** this study,we introduced a standardized process for all integrations,and described how users can utilize these models to gain insights into *** is freely accessible at https://***.

关键词： Genetic model Pharmacogenetics anticancer drug Cancer drug response

Chemotherapy as a component of multimodal therapy for gastric carcinoma

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World Journal of Gastroenterology 2006年第13期12卷 2000-2005页

作者： Yasuhiro Kodera Michitaka Fujiwara Masahiko Koike Akimasa Nakao Department of Surgery Ⅱ Nagoya University Graduate School of Medicine 65Tsurumai-choShowa-kuNagoyaAichi 466-8550Japan

Prognosis of locally advanced gastric cancer remains poor, and several multimodality strategies involving surgery, chemotherapy, and radiation have been tested in clinical trials. Phase Ⅲ trial testing the benefit of postoperative adjuvant chemotherapy over treatment with surgery alone have revealed little impact on survival, with the exception of some small trials in Western nations. A large trial from the United States exploring postoperative chemoradiation was the first major success in this category. Results from Japanese trials suggest that moderate chemotherapy with oral fluoropyrimidines may be effective against less-advanced （T2-stage） cancer, although another confirmative trial is needed to prove this point. Investigators have recently turned to neoadjuvant chemotherapy, and some promising results have been reported from phase Ⅱ trials using active drug combinations. In 2005, a large phase Ⅲ trial testing preand postoperative chemotherapy has proven its survival benefit for resectable gastric cancer. Since the rate of pathologic complete response is considered to affect treatment results of this strategy, neoadjuvant chemoradiation that further increases the incidence of pathologic complete response could be a breakthrough, and phase Ⅲ studies testing this strategy may be warranted in the near future.

关键词： Surgery Radiation anticancer drug Adjuvant chemotherapy Neoadjuvant chemotherapy

Intrinsic apoptotic pathway and G2/M cell cycle arrest involved in tubeimoside I-induced EC109 cell death

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Chinese Journal of Cancer Research 2013年第3期25卷 312-321页

作者： Yang Xu Guanghui Wang Quancheng Chen Ting Lin Zhiping Zeng Qiang Luo Jie Liu Cuiling Sun School of Pharmaceutical Sciences Xiamen University

Objective： Squamous esophageal carcinoma is highly prevalent in developing countries, especially in China. Tu Bei Mu （TBM）, a traditional folk medicine, has been used to treat esophageal squamous cell carcinoma （ESCC） for a long term. tubeimoside I （TBMS1） is the main component of TBM, exhibiting great anticancer potential. In this study, we investigated the mechanism of TBMS1 cytotoxic effect on EC109 cells. Methods： Comparative nuclear proteomic approach was applied in the current study and we identified several altered protein spots. Further biochemical studies were carried out to detect the mitochondrial membrane potential, cell cycle and corresponding proteins＇ expression and location. Results： Subcellular proteomic study in the nucleus from EC109 cells revealed that altered proteins were associated with mitochondrial function and cell proliferation. Further biochemical studies showed that TBMSl-induced molecular events were related to mitochondria-induced intrinsic apoptosis and P21-cyclin B 1/cdc2 complex-related G2/M cell cycle arrest. Conclusions： Considering the conventional application of TBM in esophageal cancer, TBMS1 therefore may have a great potential as a chemotherapeutic drug candidate for ESCC.

关键词： anticancer drug G2/M cell cycle arrest intrinsic apoptosis subcellular proteomics and tubeimoside I(TBMS 1)

Carbohydrate-based drugs launched during 2000-2021

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Acta Pharmaceutica Sinica B 2022年第10期12卷 3783-3821页

作者： Xin Cao Xiaojing Du Heng Jiao Quanlin An Ruoxue Chen Pengfei Fang Jing Wang Biao Yu Zhongshan Hospital Institute of Clinical Science Fudan University Shanghai Medical CollegeShanghai 200032China State Key Laboratory of Bio-organic and Natural Products Chemistry Center for Excellence in Molecular SynthesisShanghai Institute of Organic ChemistryChinese Academy of SciencesShanghai 200032China

Carbohydrates are fundamental molecules involved in nearly all aspects of lives,such as being involved in formating the genetic and energy materials,supporting the structure of organisms,constituting invasion and host defense systems,and forming antibiotics secondary *** naturally occurring carbohydrates and their derivatives have been extensively studied as therapeutic agents for the treatment of various *** 2000 to 2021,totally 54 carbohydrate-based drugs which contain carbohydrate moities as the major structural units have been approved as drugs or diagnostic *** we provide a comprehensive review on the chemical structures,activities,and clinical trial results of these carbohydrate-based drugs,which are categorized by their indications into antiviral drugs,antibacterial/antiparasitic drugs,anticancer drugs,antidiabetics drugs,cardiovascular drugs,nervous system drugs,and other agents.

关键词： Carbohydrate-based drug Glycodrug Glycoconjugate Antibiotics Antivirus drug anticancer drug

Effect of Nicotinamide on 12-O-tetradecanoyl-phorbol-13-acetate Exposed Mouse Skin Endonuclease Activity and DNA Synthesis

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Biomedical and Environmental Sciences 2000年第2期13卷 122-130页

作者： KRISINAP．GUPTA REENARANI CorrespondingAuthor：industrialToxicologyResearchCentre PostBOxNo.80MahatmaGandhiMargLucknow－226001India. EnvironmentalCarcinogenesisDivision IndustrialToxicologyResearchCentreLucknow

Nicotinamide (NA), a relatively nontoxic compound, has been shown to inhibit tumor development, induce differentiation, increase the sensitization of the anticancer drug resistant cancer cells and is being used in different skin ailments. But there are not many reports on its mechanism of action. Here we report that NA induced endonuclease activity. This endonuclease induction by NA appeared to be dose dependent and a function of time. As evident by the use of modifiers of DNase I, this endonuclease appeared to be like DNase type I. Increased [3H] thymidine incorporation in DNA in the presence of NA is possibly a consequence of increased 3_OH'nicks due to increased DNA fragmentation by increased endonuclease activity. The present results would be of help in the better understanding of the mechanism of NA action and its improved use in cancer control.

关键词： mechanism of action DNA fragmentation anticancer drug used in