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检索条件"任意字段=2014年中国药物制剂大会——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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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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Folate-polyethyleneimine functionalized mesoporous carbon nanoparticles for enhancing oral bioavailability of paclitaxel

Folate-polyethyleneimine functionalized mesoporous carbon na...

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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： Long Wan Qinfu Zhao Yikun Gao Ning Han Ying Wang Tongying Jiang Siling Wang Department of Pharmaceutics School of PharmacyShenyang Pharmaceutical University

Polymer-functionalized carbon nanoparticles hold great promise for their use in enhancing the oral absorption of drugs with poor oral bioavaibility. And,since the abundant expression of folate receptors in intestinal tract, folic acid(FA) modified uniform mesoporous carbon spheres(UMCS) was used to improve oral absorption of paclitaxel, a chemotherapeutic drug with poor oral bioavailability. In this research,fo late-polyethylene imine(FA-PEI) was grafted onto acid-treated uniform mesoporous carbon spheres through one-step electrostatic attraction PTX was loaded into mesopores of nanoparticles through solvent evaporation^ present as amorphous. The release of PTX from the FA-PEI-UMCS nanoparticles exhibited an initial rapid release,followed by a sustained release. And, release rate could be regulated by changing amount of FA-PEI conplex on the UMCS. The uptake of PTX-encapsulated nanoparticles was studied exploiting Caco-2 cells as an in vitro model. The results of confocal microscopy and flow cytometry demonstrated that folate fonctionalization enhanced internalization of nanoparticles by the cells. Moreover, PTX loded in FA-PEI-UMCS nanoparticles resulted in a 5.37-fold increase in apparent permeability(Papp) across Caco-2 cell monolayers compared to Taxol. In conclusion, the results of this study suggest that fo late-polyethylene imine functionalized mesoporous carbon nanoparticles have the potential to improve oral absorption of drugs with poor oral bioavailability.

关键词： Folate-polyethyleneimine functionalized mesoporous carbon nanoparticles for enhancing oral bioavailability of paclitaxel

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Programmed hydrolysis in designing paclitaxel prodrug for nanocarrier assembly

Programmed hydrolysis in designing paclitaxel prodrug for na...

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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： Qiang Fu Yongjun Wang Yan Ma John K Fallon Xinggang Yang Zhonggui He Dan Liu Feng Liu Shenyang Pharmaceutical University Guangzhou University of Chinese Medicine University of North Carolina at Chapel Hill Chapel HillNC 27599US

Nanocarriers delivering prodrugs are important strategies to improve the in vivo effectiveness and *** therapeutical efficacy,the prodrug must hydrolyze to its parent drug after administratioa In this study,we present proof-of-concept and methodology in support of our hypothesis that increased steric hindrance and decreased polarity are major handicaps for *** hypothesis has been tested using different compounds that we have *** on this discovery,we designed and synthesized PTX-S-S-Ve,PTX conjugated with Ve via disulfide *** prodrug possessed the following advantages:first,it could be encapsulated in the Ve o/w nanoemulsions(NES) because of favourable compatibility between the prodrug and nanocarrier;secondly,the PTX-S-S-Ve/Ve NES will be long-circulated in the blood in that the Ve group in the prodrug and Ve oil were molecularly matched;finally,the concentrated glutathione in the tumor microenvironment could cleave the disulfide bond and relieve the steric hindrance effect,producing an intermediate product with higher polarity,which would be further hydrolyzed to *** was demonstrated that the in vitro hydrolysis for PTX-S-S-Ve was enhanced and the cytotoxicity was *** in vivo distribution for PTX-S-S-Ve nanoemulsions varied a lot from that for PTX-Ve(ester bond)*** anticancer activity against KB-3-1 cell line was increased and the tumor was diminished after the 4th injection.

关键词： paclitaxel prodrug linker ester bond disulfide bond programmed hydrolysis cytotoxicity anticancer activity

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Anti-EGFR mAb modified cationic liposomes enhanced cellular uptake of survivin-siRNA

Anti-EGFR mAb modified cationic liposomes enhanced cellular ...

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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： Pan Shen Ying Lin Qing-Ri Cao Jing-Hao Cui College of Pharmaceutical Science Soochow University

In order to prepare dry powder inhalation for pulmonary delivery of siRNA for lung cancer therapy,the effect of Anti-EGFR mAb modification and cationization of survivin-siRNA baded liposome on the cellular uptake of A549/DDP was *** physicochemical properties and cytotoxicity of carriers as well as the cellular uptake and apoptosis were observed,*** results,as a novel cationization agent,staramine and DSPE-PEG2000-Mal were successfully synthesized with relative high purity as 87.0%and 86.2%,*** average size and zeta potential of EGFR-PEG-SCLs-siRNA were(172.7±6.6) nm and(+7.78±0.5) *** entrapment efficiency of siRNA was(90.8±0.8)%.Liposomes can protect siRNA from degradation from RNase in *** force microscopy(AFM) was used to observe the endocytosis of ***-EGFR mAb modification increased significantly cellular uptake as its mean fluorescence intensity was 1.4-fold higher by Fbw *** results of uptake pathways of EGFR-PEG-SCLs indicated that clathrin-mediated endocytosis and caveolin-mediated endocytosis were the major routes with energy *** apoptotic Index of A549/DDP cells incubated with EGFR-PEG-SCLs-siRNA group was(41.19±1.83)%,significantly higher than that in Lipofectamine-2000 transfection group(42.84 ± 2.53)%.In conclusion,the modification of survivin-siRNA loaded liposomes with Staramine and Anti-EGFR mAb could improve significantly cellular of A549/DDP with low cytotoxicity which shows the meaningful potential for its application in pulmonary delivery.

关键词： Survivin-siRNA cationic liposomes cellular uptake

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Cationic charged N-(2-hydroxypropyl) methacrylamide copolymer-based strategy for overcoming the folate dilemma

Cationic charged N-(2-hydroxypropyl) methacrylamide copolyme...

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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： Lian Li Qingqing Yang Zhou Zhou Jiaju Zhong Yuan Huang Key Laboratory of Drug Targeting and Drug Delivery System Ministry of EducationWest China School of PharmacySichuan University

Although folate exhibits many advantages over other targeting ligands,it has one major defect:poor water *** it was conjugated to hydrophilic drug carrier such as N-(2-hy droxypropyl) methacrylamide(HPMA) copolymer,the hydrophobic folate may be buried inside the random polymer coil and not exposed to be accessible to its receptor on the cell surlace,thus losing its active targeting *** address this folate dilemma,the positive charge was introduced in the present *** obtained cationic folate-functionalized HPMA copolymers exhibited a synergistic enhancing effect on cellular uptake by folate receptor(FR) positive Hela cells via electrostatic absorptive endocytosis and folate receptor mediated endocytosis,with the involvement of multiple internalization pathways including clathrin-mediated endocytosis,caveolae-mediated endocytosis,macropinocytosis and energy-dependent *** demonstrated in binding efficiency study,the FR antibody bound to 71.2%of tested cells in the competition with neutral folate modified HPMA copolymers,while the FR antibody bounded cells decreased to only 34.0%in competition with cationic folate modified HPMA copolymers,indicating that the positively charge could probably amplify the binding efficiency of folate to its receptor due to close proximity of the conjugates to the cell surface by the electronic adhesioa In addition,the cell uptake study on FR negative A549 cells also confirmed the specific role of folate as targeting ligand.

关键词： HPMA copolymer active targeting folate dilemma

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Study on Preparation Technology of Sustained-release Dropping Pills of Trimebutine Maleate

Study on Preparation Technology of Sustained-release Droppin...

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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： WANG Jun-jun DONG Xiao-lei HUANG Sheng-wu Zhejiang Chinese Medical University Beingmate Group Co. Ltd

OBJECTIVE According to the feature that Trimebutine Maleate has poor aqueous solubility,low bioavailability when taken orally,short biological half-life(2.7h),sustained-release dropping pills were prepared to achieve release slowly,reduce the bbod drug concentration fluctuations and decrease frequency of *** Polyethylene glycol,stearic acid and glycerin monostearate were used as matrix to prepare trimebutine maleate sustained-release dropping pills by melting *** liquidity,difficulty Level of preparation,settling velocity and roundness were used as evaluation indexes to conduct preliminary prescription *** optimal formulation was selected with interval optimization method of releasing degree by dissolution *** optimum technology was finally confirmed in orthogonal test by comprehensive scores including roundness,pills weight difference and accumulative *** The proportion of prescription was TM:PEG4000:PEG6000:SA:GMS= 2.4:1.2:1.2:1.2:1.2,the optimum technological condition:the temperature of drug liquid was 75℃,the freezing temperature was30→℃,the distance to the condensed fluid was 5 *** behavior in vitro of trimebutine maleate sustained-release dropping pills accorded with first order equation and Hugich *** Formability of trimebutine Maleate sustained-release dropping pills was good,release behavior in vitro was slow,blood drug concentration fluctuations was decreased and frequency of use was reduced,trimebutine Maleate sustained-release dropping pills with this method meet the clinical needs.

关键词： Trimebutine maleate sustained-release dropping pills moulding techniques release behavior in vitro

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Targeted delivery of doxorubicin and combretastatin A4 via a two-in-one liposomal system(TWOLips) for antineoplastic combination therapy

Targeted delivery of doxorubicin and combretastatin A4 via 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： Tingting Su Yingying Long Chunyue Deng Xiaolin Zhang Zhangbao Chen Chong Li College of Pharmaceutical Sciences Southwest University Key Laboratory of Smart Drug Delivery Ministry of Education and PLASchool of PharmacyFudan University

There is an increasing need for improved methods to deliver combination and/or multi-drug therapies to treat malignant *** contrast to other work that takes a 'start-from-zero' approach,we constructed a novel two-in-one liposomal system(TWOLips) assembled from two single drug-loaded *** results demonstrated that TWOLips can be prepared via an easy and mild process,through silica coating and incubation with *** had a mean diameter of 100 nm,relatively high drug loading rates(96.8±0.9%for doxorubicin and78.4±1.2%for combretastatin),and high storage *** of TWOLips with a targeting moiety comprised of an all D-amino acid peptide derived from natural VEGF resulted in strong and selective binding to VEGFR2,a marker of tumorigenesis,in vitro and in *** growth and angiogenesis were significantly inhibited and survival was enhanced in A375 melanoma xenograft-bearing mice treated with the TWOLips system Further,the TWOLips system had a low potential risk of *** the 'liposome-by-liposome' assembly can be further cycled,TWOLips shows a promising potential for the treatment malignant tumors,especially those that require multiple drugs.

关键词： combination therapy RIV VEGFR2 doxorubicin combretastatin A4

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Development of a novel Tanshinone Ⅱ A sustained-release coated pellets based chronotherapy of angina pectoris and deconvolution

Development of a novel Tanshinone Ⅱ A sustained-release coa...

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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： Hong-xiang Yan Zheng-hua Li Wen-li Zhang Jian-ping Liu Pharmaceutical Institute China Pharmaceutical University

The aim of this study was to develop and optimize the coating formulation for nTanshinone Ⅱ A(TA) sustained-re lease pellets in order to meet the needs of clinical application The plasma concentration-time curve of TA oral ternary solid dispersion pellets in New Zealand White rabbits(weight function) was *** predicted(expected) plasma concentration-time curve of TA(response function)was simulated according to the incidence of angina pectoris in 24 *** desired release pattern(input function) was calculated using deconvolution ***,developed from TA ternary solid dispersion pellets,a series of TA sustained-re lease coated pellets were prepared by utilizing fluid-bed coating *** vitro release test showed that the profile of optimal coating formulation was closely analogous to the desired *** vivo study and data analysis demonstrated there had no statistically significant difference for Tmax and MRT values(approximate 10 h and 17 h,respectively) between the observed and predicted plasma concentration-time curves,confirming that in vivo pharmacokinetic performance of TA sustained-re lease coated pellets was consistent with the predicted *** conclusion,deconvolution can be employed in the development the TA sustained-release coated pellets,which presents a more rational in vivo process with an improvement in the therapeutic effectiveness.

关键词： Tanshinone Ⅱ A pellets deconvolution sustained-release coating pharmacokinetics similarity factor(f2)

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Targeting multifunctional nanoparticles based on dual pH-responsive and CD44receptor for anticancer delivery

Targeting multifunctional nanoparticles based on dual pH-res...

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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： Daquan Chen Kaoxiang Sun Wanhui Liu Youxin Li Zimei Wu School of Pharmacy Yantai UniversityShandong Collaborative Innovation Center of new pharmaceutical preparations and biotech drug State Key Laboratory of Long-acting and Targeting Drug Delivery System

In this article,we prepared a multifunctional oligosaccharides of hyaluronan(oHA) conjugates,oHA-histidine-menthone 1,2-glycerol ketal(oHM).The oHM conjugates possess pH-sensitive menthone 1,2-glycerol ketal(MGK) as hydrophobic moieties and oHA as the target of CD44 *** polymeric mPEG-Chitosan-Ketal(PCK) carrying pH-sensitive ketal group as hydrophobic moieties and PEG group as hydrophilic moieties were *** two pH-sensitive ketal derivatives were employed to fabricate nanoparticles for antitumor drug *** oHM-PCK nanoparticles(oHPN) can spontaneously self-assemble into mixed micellar structure with nano-sized spherical shape of 100-200 nm at pH 7.4PBS *** oHPN could release encapsulated curcumin with 92.6%at pH 5.0compared with 55.3%at pH *** results of cytotoxicity assay indicated that encapsulated curcumin in oHPN(Cur-oHPN) have less toxicity compared to curcumin *** anti-tumor efficacy in vivo suggested that Cur-oHPN suppressed tumor growth most *** results present the promising potential of oHPN as a new and effective nano-sized pH-sensitive drug delivery system

关键词： dual pH-sensitive multifunctional 1 2-glycerol ketal(oHM) PCK nanoparticles

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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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