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检索条件"任意字段=2014中国药物制剂大会——中国药学会药剂专业委员会年会、第六届亚洲阿登制药技术研讨会暨国际控释协会中国分会年会"

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Effects of PLGA nanoparticles with different sizes on rat hepatic cytochrome P450 enzymes activities

Effects of PLGA nanoparticles with different sizes on rat he...

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2014中国药物制剂大会——中国药学会药剂专业委员会年会、第六届亚洲阿登制药技术研讨会暨国际控释协会中国分会年会

作者： Xuan He Lihui Qiu Ruiqi Qiu Jiangeng Huang Gao Li Luqin Si The School of Pharmacy Tongji Medical CollegeHuazhong University of Science and Technology

Objective:There are very little available reports about the interaction of PLGA nanoparticle with cytochrome P450 *** aim of this study was to investigate the inhibitory effects of PLGA nanoparticles with different sizes on rat hepatic cytochrome P450 enzymes(CYP1 A,CYP3 A,CYP2B,CYP2 D,CYP2C) ***:The inhibitory effects of PLGA nanoparticles(0.1,0.2,0.4,0.6,0.8,1.0mg/mL) on the major rat hepatic cytochrome P450 enzymes(CYP1A,CYP3 A,CYP2B,CYP2 D,CYP2C) activities were examined using rat liver ***(CYP3A),testosterone(CYP3A),phenacetin(CYP1A),tolbutamide(CYP2C),S-mephenytoin(CYP2C) and dextromethorphan(CYP2D) were selected as probe substrates,***:Five different sizes of PLGA NPs with mean particle sizes of around 60 nm(name as PLGA NPs-1),110 nm(name as PLGANPs-2),150 nm(name as PLGA NPs-3),300 nm(name as PLGA NPs-4) and 450 nm(name as PLGA NPs-5) were *** polydispersity indexs(PDI) were all less than 0.2,and the zeta potential was between-3 and-36 *** IC50 values for these five different sizes PLGANPs on CYP 2C,CYP2 D,CYP3 A(testosterone was used as probe substrates) were all more than 1 mg/mL indicating that PLGA NPs had no inhibitory effect on tolbutamide4-hydroxylase,(S)-mephenytoin 4-hydroxylase,dextromethorphan O-demethylase and testosterone 6β-*** CYP 1A and CYP3A(midazolam was chosed as probe substrates),only the IC50 values of PLGA NPs-4(IC50=0.6331 mg/mL for CYP3A) and PLGA NPs-5(IC50=0.8972 mg/mL for CYP1 A,IC50=0.9667 mg/mL for CYP3A) were less than 1 mg/mL,which indicated larger PLGA NPs had some influence but not small ones(PLGANPs-1,2,3).When the concentration of PLGANPs reached 1 mg/mL,the remain activities of CYP1A(not for PLGA NPs-4),CYP3 A,CYP2B,CYP2 D,CYP2C by PLGA NPs-4 and PLGA NPs-5 were significantly decreased compared with PLGANPs-1,PLGANPs-2,PLGA NPs-3,***:PLGA nanoparticles cannot inhibit the metabohsm of xenobiotics by the CYP450 system in rat

关键词： PLGA nanoparticles Cytochrome P450 enzyme Liver microsome IC50

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Systemic delivery of paclitaxel using N-succinyl-palmitoyl-chitosan micelles decorated with cRGDyK peptide inhibit Orthotopic Non-Small-Cell Lung Cancer

Systemic delivery of paclitaxel using N-succinyl-palmitoyl-c...

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2014中国药物制剂大会——中国药学会药剂专业委员会年会、第六届亚洲阿登制药技术研讨会暨国际控释协会中国分会年会

作者：袁志强 Wei-liang Chen Shu-di Yang Xue-nong Zhang 苏州大学药学院 Department of Pharmaceutics College of Pharmaceutical ScienceSoochow University

BACKGROUND:In the treatment of human non-small-cell lung cancer(NSCLC),intravenous administration makes drugs accumulate not only in the lungs but also in other organs and may undergo degradation in the systemic circu... 详细信息

关键词： PTX Systemic delivery of paclitaxel using N-succinyl-palmitoyl-chitosan micelles decorated with cRGDyK peptide inhibit Orthotopic Non-Small-Cell Lung Cancer

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Bubble-Generating Carrier Systems for Localized Controlled Release

Bubble-Generating Carrier Systems for Localized Controlled R...

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2014中国药物制剂大会——中国药学会药剂专业委员会年会、第六届亚洲阿登制药技术研讨会暨国际控释协会中国分会年会

作者：宋信文 Ko-Jie Chen Ming-Fan Chung Chun-Wen Hsiao Zi-Xian Liao Wei-Tso Chia Kun-Ju Lin Department of Chemical Engineering National Tsing Hua University Institute of Biomedical Engineering National TsingHua University Department of Orthopedics National Taiwan University Hospital Hsinchu Branch Molecular Imaging Center Chang Gung Memorial Hospital Department of Medical Imaging and Radiological Sciences Chang Gung University

In this work,two bubble-generating agents,ammonium bicarbonate(ABC)and sodium bicarbonate(SBC)that can generate CO2 bubbles,are separately encapsulated in carrier systems for actively triggering drug release *** recog... 详细信息

关键词： SBC Bubble-Generating Carrier Systems for Localized Controlled Release

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Preparation and evaluation of phospholipid complex based microemulsion for oral delivery of insulin

Preparation and evaluation of phospholipid complex based mic...

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2014中国药物制剂大会——中国药学会药剂专业委员会年会、第六届亚洲阿登制药技术研讨会暨国际控释协会中国分会年会

作者：胡雄彬 Xiuling Lu Tiantian Tang 向大雄中南大学湘雅二医院 Institute of Clinical Pharmacy Central South University Department of Pharmacy the Second Xiangya HospitalCentral South University

The present work explored the possibility of formulating oral insulin delivery system by combing the advantage of microemulsion and phospholipid *** phospholipid complex(IPC) was prepared by an anhydrous co-solvent lyophilization *** parameters affecting formulation were *** preparation has unimodal particle size distribution with a mean diameter of27.3±0.2nm The results of bioactivity evaluation indicated that insulin was able to withstand the preparation *** was protected from enzymes by incorporation into oil *** IPC-microemulsion was effective in enhancing insulin transport across caco-2 cell *** IPC-microemulsion especially the IPC-W/O microemulsion was effective in reducing bbod glucose level in diabetic animal *** complex based microemulsion appear to be an interesting candidate for oral delivery of insulin.

关键词： Insulin Phospholipid complex Microemulsion

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Assembly of Pharmaceutical Micro particles via Spray Drying

Assembly of Pharmaceutical Micro particles via Spray Drying

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2014中国药物制剂大会——中国药学会药剂专业委员会年会、第六届亚洲阿登制药技术研讨会暨国际控释协会中国分会年会

作者：柳文洁 Zeneng Cheng Xiao Dong Chen School of Pharmaceutical Sciences Central South University College of Chemistry Chemical Engineering and Materials ScienceSoochow University

Pharmaceutical microparticles require stringent control over their characteristics to realize their optimal therapeutic *** drying represents an elegant one-step route for the production of pharmaceutical microparticles,although a typical feature of conventional spray-dried products is the significant variation in particle ***,the synthesis of pharmaceutical microparticles with homogeneous characteristics is possible with a micro-fluidic jet spray drying *** progress fecilitates the methodical study on the direct relationship among formulation,production,physicochemical properties,and functionalities of these pharmaceutical microparticles via the spray-drying *** examples on the design and assembly of microparticles with tailor-made properties and functionalities are presented,with specific emphasis on the control over particle size,shape,microstructures,and controlled release *** underlying particle formation mechanisms and design concepts presented here are not limited to pharmaceutical components but to other functional particles as well.

关键词： pharmaceutical particles micro-fluidic jet spray drying microstructure controlled release

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Applications of Cell-Penetrating Peptides in Delivery of Macromolecular Drug for Cancer Treatment

Applications of Cell-Penetrating Peptides in Delivery of Mac...

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2014中国药物制剂大会——中国药学会药剂专业委员会年会、第六届亚洲阿登制药技术研讨会暨国际控释协会中国分会年会

作者： Victor C.Yang Pharmaceutical Sciences College of Pharmacy University of Michigan Department of Molecular Medicine and Biopharmaceutical Sciences Seoul National University

One of the major obstacle in achieving effective tumor drug therapy is the membrane barrier of tumor cells that is permeable to only small(<700 Da) and hydrophobic *** most widely used method to-date in achieving intracellular drug delivery is via the receptor-mediated *** cell-entry method,however,requires invagination and vasculation of the membrane Up id bilayer to form free cytoplasmic *** large drugs such as proteins that have entered this pathway remain enclosed within the lipid vesicles,they do not have access to the cell cytoplasm;a pre-requisite for such drugs to exert cytotoxic *** counter this obstacle,we proposed a novel strategy by linking the macromolecular drug with LMWP,a potent yet non-toxic cell-penetrating peptide(CPP) developed in our *** studies demonstrated that by covalently linking CPP to almost any type of drugs(***) or carriers(***),CPP was able to ferry the attached cargos into all organ/tissue types including the brain,without causing membrane perturbation or cytotoxicities.A wide variety of applications of LMWP in attaining intracellular drug delivery for cancer treatment will be discussed in this presentation

关键词： Applications of Cell-Penetrating Peptides in Delivery of Macromolecular Drug for Cancer Treatment

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In vivo delivery of exenatide with mesoporous silicon nanoparticles as vehicles

In vivo delivery of exenatide with mesoporous silicon nanopa...

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2014中国药物制剂大会——中国药学会药剂专业委员会年会、第六届亚洲阿登制药技术研讨会暨国际控释协会中国分会年会

作者：徐骏军 Guowei Wang Manman Guo Weidong Fei 李范珠浙江中医药大学药学院 College of Pharmaceutical Science Zhejiang Chinese Medical University

Purpose A subcutaneous exenatide delivery system was devebped to achieve sustained release via mesoporous silicon *** Exenatide was loaded into mesoporous silicon *** vitro,EXT@SBA-15 release was investigated by *** vivo,EXT plasma concentrations were analyzed after delivery in *** they were determined using the exendin-4 EI A *** use diabetic mice to monitor bbod *** The morphology of EXT@SBA-15 was *** mean particle size,drug loading and entrapment efficiency were(920±120) nm,(15.23±2.0)%,(***.30)%,*** in vitro release profiles of the EXT@SBA-15 in PBS buffer atpH 7.4was expressed well by First order *** pharmacokinetic profiles showed that EXT@SBA-15 can be sustained release than EXT-SoL Compared with model control group,EXT@SBA-15 can control blood glucose obviously within 10 days,and it can control blood glucose more stable than EXT-Sol which subcutaneous injection twice a *** A subcutaneous exenatide delivery system was devebped and characterized in vitro and in vivo and it represents a promising sustained and tailorable release system for exenatide.

关键词： In vivo delivery of exenatide with mesoporous silicon nanoparticles as vehicles SBA

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Hydrazone Containing PEG-Hz-PLA Micelles as pH-Responsive Delivery Vehicles for Anticancer Drug

Hydrazone Containing PEG-Hz-PLA Micelles as pH-Responsive De...

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2014中国药物制剂大会——中国药学会药剂专业委员会年会、第六届亚洲阿登制药技术研讨会暨国际控释协会中国分会年会

作者： Jing Xu Yongqiang Bu 宋仕永 Pharmaceutical College of Henan University 河南省开封市河南大学药学院

The pH-responsive micelles for the dehvery anticancer agents have been found great potential in the past *** acid labile hydrazine bonds were formed by conjugating DOX onto side *** other drugs such as Paclitaxel(PTX) and cisplatin are not applicable for the lack of special functional *** this study,diblock ***(ethylene glycol)-hydrazone-poly(lactic acid)(PEG-Hz-PLA) containing pH-responsive hydrazone bond between hydrophilic and hydrophobic segments were *** pH-sensitive biodegradable micelles were fabricated and used as anticancer drug dehvery *** Light Scattering(DLS) measurements show that PEG-Hz-PLA self-assemble into micelles with an average diameter of ca.74 nm and size change in acidic solutions,while remaining unchanged in phosphate buffer with a pH value of *** were observed when the micelles dispersed in acetate buffer(10 mM,pH4.0) as a result of cleaving of the hydrophilic *** was used as a modle drug loaded into the micells and the drug loading content was 2.9%.In vitro release studies showed that PTX steadily released from drug-toaded PEG-Hz-PLA micelles in 24 *** release of PTX was significantly expedited at pH 4.0 and pH 5.0 in 24 *** pH responsive degradable PEG-Hz-PLA micelles may serve as a promising drug dehvery system for the dehvery of all kinds of anti-cancer drugs.

关键词： PEG-Hz-PLA Paclitaxel mecelles pH-sensitive

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Injectable long-acting sustained release drug formulations and industrialization

Injectable long-acting sustained release drug formulations a...

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2014中国药物制剂大会——中国药学会药剂专业委员会年会、第六届亚洲阿登制药技术研讨会暨国际控释协会中国分会年会

作者：孙考祥 Wanhui Liu Youxin Li 绿叶制药集团研发中心烟台大学药学院

Sustained and controlled release formulations which is local injection administered once a few weeks or months has been highly concerned by a great number of pharmaceutical researchers and companies,especially important for long-term medication diseases as cancer,diabetes,mental illness and neurodegenerative *** drug delivery system has several advantages:1) Injected directly into the lesion,reduce adverse reactions and increase the therapeutic effect;2) Reduce the frequency of administration and improve patient compliance significantly;3) Control the drug sustained release in several weeks or months which could make the drug plasma concentration flatten,reduce drug plasma concentration fluctuations by administered conventional formulations repeatedly and improve the safety and effectiveness of drugs;4) From the point of view of pharmacoeconomics,it can significantly reduce treatment costs and improve value.5) Further patent applications,help manufacturers to extend the life of the drug *** the past few decades,there have been some important long-acting injectable formulations marketed,such as injectable implants,microspheres,in situ gel and nano-suspensions,*** have been a large amount of literatures published about long-acting sustain and controlled release formulations,but most are prepared in laboratory *** from the laboratory production to industrial production is still face a variety of *** presentation will discuss and focus on the progress of product development of injectable long-acting sustainedrelease formulations,from the perspective of industrialization and combined with practice of Luye Pharmaceutical Group's product development.

关键词： Injectable long-acting sustained release drug formulations and industrialization

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Functional targeting drug liposomes and the treatment of brain glioma

Functional targeting drug liposomes and the treatment of bra...

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2014中国药物制剂大会——中国药学会药剂专业委员会年会、第六届亚洲阿登制药技术研讨会暨国际控释协会中国分会年会

作者： Xiu-Ying Li 吕万良 School of Pharmaceutical Sciences at Peking University 北京大学药学院药剂学系

Invasive brain glioma is the most lethal type of cancer and is highly *** leads to an extremely poor prognosis and makes complete surgical removal of the tumor virtually ***-penetration of therapeutic drugs across the blood-brain barrier(BBB),brain cancer stem cells(CSCs),and brain cancer vasculogenic mimicry(VM) results in relapse after surgical and radio *** developed a functional targeting chemotherapy for transporting drugs across the BBB,destroying VM channels,and eliminating CSCs and cancer cells in the *** studies were undertaken on brain glioma cells in vitro and in brain glioma-bearing *** paclitaxel as the anticancer drug and artemether as the regulator of apoptosis and inhibitor of VM channels,a kind of functional targeting paclitaxel plus artemether liposomes was developed by modifying two new functional materials:a mannose-vitamin E derivative conjugate(MAN-TPGS1000) and a dequalinium-lipid derivative conjugate(DQA-PEG2000-DSPE).The transport mechanism across the BBB was associated with receptor-mediated endocytosis by MAN-TPGS1000 conjugate via glucose transporters and adsorptive-mediated endocytosis by DQA-PEG2000-DSPE conjugate via electric charge-based *** efficacy was related to the destruction of VM channels by regulating VM indicators,as well as the induction of apoptosis in brain cancer cells and CSCs by activating apoptotic enzymes and pro-apoptotic proteins and inhibiting anti-apoptotic *** data suggest that the chemotherapy using functional targeting paclitaxel plus artemether liposomes could provide a new strategy for treating invasive brain glioma.

关键词： Functional targeting liposomes brain glioma cancer stem cells VM channels anticancer efficacy

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