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检索条件"任意字段=2012年中国药物制剂大会——中国药学会药剂专业委员会年会、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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Self-assembled Methoxy Poly(ethylene glycol)-Cholesterol Micelles for Hydrophobic Drug Delivery

Self-assembled Methoxy Poly(ethylene glycol)-Cholesterol Mic...

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2012年中国药物制剂大会——中国药学会药剂专业委员会年会、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： Yiyi Yu Gu He Xiangrong Song Yingju He Bei Xu Zhiyao He Ying Zhang Yan Chen Yang Yang Yongmei Xie Yu Zheng State Key Laboratory of Biotherapy West China HospitalSichuan UniversityChengduSichuan 610041Chi West China School of Pharmacy Sichuan UniversityChengduSichuan 610041China School of Pharmaceutical Science & Yunnan Key Laboratory of Pharmacology for Natural Products Kunmin

Objective:to promote the application of methoxy poly (ethylene glycol)-cholesterol (mPEG-CHOL) in hydrophobic drugs loading,mPEG-CHOL was used to prepare core-shell micelles (DTX-PM) encapsulating docetaxel (DTX) with poor water solubility by modified co-solvent evaporation ***:approaches investigated for the enhancement of DTX entrapment efficiency (EE) and the minimization of particle size included the organic and aqueous phase composing,the organic/aqueous phase volume ratio and the polymer concentration (Fig.1).The optimal DTX-PM was characterized by dynamic light scattering (DLS),transmission electron microscopy (TEM) and differential scanning calorimetry (DSC),besides storage stability and in vitro cytotoxicity assay.

关键词： Co-solvent evaporation Methoxy poly (ethylene glycol) Cholesterol Polymer Micelles Docetaxel Stability Hydrophobic drug

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G3-C12 peptide as a novel kidney renal targeting drug carrier

G3-C12 peptide as a novel kidney renal targeting drug carrie...

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2012年中国药物制剂大会——中国药学会药剂专业委员会年会、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： Qian Geng,Tao Gong,Xun Sun,Zhirong Zhang~* Key Laboratory of Drug Targeting and Drug Delivery Systems,Ministry of Education,West China School of Pharmacy,Sichuan University,Chengdu,People's Republic of China.

Chronic kidney disease(CKD)is increasingly recognized as a major public health *** targeting delivery to the kidney is an attractive method to increase the drug efficacy,as this approach will generate higher renal drug *** extensively used as vehicles of radioactivity for targeted imaging and radiolabeled peptides also caused high and persistent localization of radioactivity in the *** addition,the renal uptake owes to the peptides carrier rather than the radiometabolite. So we propose these peptides can be used as vehicle to delivery therapeutic agents to the kidney by synthetic drug-carrier conjugate with definite structure and high purity in solid phase by the renal reabsorption of the peptide.G3-C12 peptide identified using combinatorial phage display technique specifically accumulate in the kidney after radiolabeled,the objective of this present study is to develop a novel peptide-drug conjugate for the targeted delivery of renal drug.

关键词： Kidney targeted drug delivery system Chronic kidney disease G3-C12 peptide Captopril Drug-carrier conjugate

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A novel method to increase release uniformity of Blossom(Venlafaxine Hydrochloride Sustained Release Tablets)

A novel method to increase release uniformity of Blossom(Ven...

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2012年中国药物制剂大会——中国药学会药剂专业委员会年会、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： Qiyu Zhang,Kun Zhang,Yan Ma,Gang Yang,Wan Wang,Xiao Ke,Qiang Zheng National recognized enterprise center,Chengdu Kanghong Pharmaceutical Co.Ltd.

Objective:To further enhance Blossom,venlafaxine hydrochloride sustained release tablet,releasing uniformity. Method:The researcher systematically studied many factors that may influence the releasing profile of Blossom ,including osmotic pressure,particle size,semi-permeable membrane thickness,core hardness,size and number of delivery *** apparatusⅡwas used to determine in vitro release. Result:An increase in accumulating releasing uniformity was observed on decreasing penetration enhancer particle size（shown in Fig.1）.The research demonstrated that the penetration enhancer particle size can affect drug release *** smaller particle size penetration enhancer can make the dissolve speed more evenly which aid to provide more constantly osmotic pressure. And osmotic pressure comes to be the main factor which influences release behavior of osmotic pump tablets（shown in Fig.2）.More data showed that using nano-size grade penetration enhancer can even make the difference between the same batch products less than 2.0%. Conclusion:Smaller particle size penetration enhancer can improve releasing rate uniformity.

关键词： Blossom venlafaxine hydrochloride releasing uniformity

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HPMA copolymer-(G3-C12)-5-Fluorouracil conjugates show improved efficacy to prostate carcinoma

HPMA copolymer-(G3-C12)-5-Fluorouracil conjugates show impro...

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2012年中国药物制剂大会——中国药学会药剂专业委员会年会、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： Yang Yang.Zhou Zhou,Shuang He,Tingting Fan,Yun Jin,Xi Zhu,Zhi-rong Zhang,Yuan Huang~* Key Laboratory of Drug Targeting and Drug Delivery System,Ministry of Education,West China School of Pharmacy,Sichuan University.No.17,Block 3,Southern Renmin Road,Chengdu 610041,P.R.China

Purpose:The aim of this study was to develop a G3-C12-mediated drug delivery system based on N-(2-hydroxypropyl) methacrylamide(HPMA) copolymers targeting to Galectin-3(Gal-3)-expressed human PC-3 prostate carcinoma cells. Method:G3-C12 peptide,which specifically binds to the carbohydrate-recognition domain(CRD) of Gal-3,was attached to HPMA copolymers as a targeting ***-3-targeted and non-targeted HPMA copolymer-5-Fluorouracil(5-Fu) conjugates were synthesized and *** in vitro cytotoxicity and subcellular fate,in vivo biodistribution and antitumor efficacy of the conjugates were investigated.

关键词： G3-C12 peptide Human PC-3 prostate carcinoma cells 5-Fluorouracil Gal-3-targeted HPMA copolymer-(G3-C12)-5-Fu conjugate

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Preparation of paeonol transdermal delivery systems based on the microemulsion-based gels and the characters of pharmacokinetics

Preparation of paeonol transdermal delivery systems based on...

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2012年中国药物制剂大会——中国药学会药剂专业委员会年会、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： LIU Ji-Yong,HAN Ying,ZHU Quan-Gang,SUN Hua-Jun,GAO Shen~* Department of pharmacy,Changhai Hospital,the Second Military Medical University,Shanghai 200433)

Objectives:To investigate the pharmacokinetics of paeonol microemulsion,microemulsion-based gels and marketed paeonol ointments by the skin-blood synchronous microdialysis coupled with LC/***:The microdialysis systems were established by linear probes and concentric circles *** vivo recovery of paeonol in skin is 69.7±4.8%and in blood is 51.6±7.2%.The paeonol microemulsion,microemulsion based gels and marketed paeonol ointments were administrated to ***（pH7.4）served as perfused *** perfused rate was 5μL·mLand the microdialysis samples were collected every 20 min *** paeonol concentration in perfused solution was determined by LC/***:Paeonol microemulsion,microemulsion-based gels significantly raised the drug concentrations in skin more than that of paeonol *** paeonol microemulsion based gels has similar bioavailability as the paeonol ointments in blood,but its blood drug concentrations were ***:The paeonol microemulsion based gels may be developed into a new preparation for dermis *** skin-blood synchronous microdialysis technique proved a new method for the pharmacokinetics study of transdermal delivery systems.

关键词： paeonol microemulsion based gels microdialysis transdermal delivery systems pharmacokinetics

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Hyaluronic acid-graft-branch polyethylenimine as a novel target specific vector in siRNA delivery

Hyaluronic acid-graft-branch polyethylenimine as a novel tar...

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2012年中国药物制剂大会——中国药学会药剂专业委员会年会、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： Ge JIANG:Yu-jiao YUAN Shool of Life science and Biotechnology,Dalian University.Dalian 116622.

Objective:To develop a novel vector for siRNA delivery with low molecular weight Polyethylenimine(PEI)grafted to the hyaluronic acid(HA). Methods:The properties of HA-PEI were characterized by *** siRNA binding ability of HA-PEI was erected by gel electrophoresis retardation *** particle size of siRNA/HA-PEI complex was measured by using *** cytotoxicity of siRNA/PEI-HA complex was evaluated by MTT *** siRNA / PEI-HA complex in vitro PGL3-Luc gene silencing efficiency was evaluated by plasmid / liposome transfection method. Results:The particle size of siRNA/HA-PEI complex was about 20 *** electrophoresis showed that at W/W ratio of 3 the polymer was able to completely condense *** cytotoxicity of siRNA/PEI-HA complex to B16F1 cells was lower than that of siRNA/PEI *** survival rate of siRNA/PEI-HA complex cell was significantly higher,and there is a higher efficiency in gene ***/PEI-HA complex appeared to silence PGL3-Luc gene in the range of 50%-85%depending on the serum concentration up to 50vol%. Conclusion:PEI-HA complex as a specific target cells siRNA carrier is promising.

关键词： hyaluronic acid polyethyleneimine siRNA carrier transfection

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Neuropilin-1-mediated liposome drug delivery system for targeted therapy of glioblastoma

Neuropilin-1-mediated liposome drug delivery system for targ...

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2012年中国药物制剂大会——中国药学会药剂专业委员会年会、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： Yiyi Yang~(1,2),Zhiqiang Yan~(2,*),Jian Zhong~2,Daixu Wei2,Dannong He1,~(2,*),Weiyue Lu~3 1 Dept.of Material science and technology,School of Material science and technology,Shanghai Jiaotong University,Shanghai 200240,PR China 2 National Engineering Research Center for Nanotechnology,Shanghai 200241,PR China 3 Key Laboratory of Smart Drug Delivery,Ministry of Education & PLA,Department of Pharmaceutics,School of Pharmacy,Fudan University,Shanghai 201203,PR China

Objective Glioblastoma shows a high incidence rate,and the life times of the patients were quite *** present,the active targeting drug delivery system cannot penetrate into the whole tumor tissue due to the poor permeability of the targeting moiety in the tumor ***-1(NRP-1) is a receptor overexpressed on both glioblastoma cells and tumor *** peptide,the specific ligand of NRP-1,is a tumor-penetrating peptide,able to penetrate through tumor vessels and tumor ***

关键词： Neuropilin-1 Tumor-penetrating peptide RGERPPR Liposomes Glioblastoma

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Optimized preparation of vinpocetine micelles and in vivo evaluation of its pharmacokinetics in rats

Optimized preparation of vinpocetine micelles and in vivo ev...

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2012年中国药物制剂大会——中国药学会药剂专业委员会年会、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： Run-Cheng Liang,Shu-Ling Huang,Xiao-Juan Guo,Yu-Ting Wang,Fan Yang~* School of Pharmacy,Guangdong Pharmaceutical University,Guangdong Guangzhou,510006,China

Objective:The aim of this study was to assess the potential of vinpocetine loaded micelles fabricated from mPEG-PLA as a sustained release system and its pharmacokinetics in ***:Three micelle fabrication methods were examined to maximize vinpocetine loading,followed by structurally characterized and investigation of in vitro release and in vivo pharmacokinetics in Sprague-Dawley *** pharmacokinetic parameters of vinpocetine in micelle formulation were compared to its clinical ***:A thin-film hydration method yielded vinpocetine loaded micelles with relatively high loading content(>20%) in nanoparticle size range(118.3 nm).The results of Fourier transform infrared(FTIR)and transmission electron microscopy(TEM) confirmed the encapsulation of vinpocetine inside the micelles *** loaded micelles exhibited a sustained release behavior up to 48 *** intraperitoneal administration(9 mg/kg),vinpocetine loaded micelles provided significantly higher(335%) plasma AUC compared to vinpocetine injection,and also increased the mean residence time[MRT(O-t)]and elimination half-life (t1/2z).Conclusion:In summary,these data demonstrate that mPEG-PLA micelles can efficiently sustain vinpocetine concentrations in plasma for 36 h,thus apprehending polymeric micelles suitability as poor aqueous solubility drug carriers.

关键词： Polymeric micelles Vinpocetine Sustained release Pharmacokinetics rats

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The effect of poly(amidoamine) Dendrimers on the transport of puerarin in human corneal epithelial cell

The effect of poly(amidoamine) Dendrimers on the transport o...

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2012年中国药物制剂大会——中国药学会药剂专业委员会年会、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： Tao Qu~1,Xiudi Zhou~1,Junhua Wei~1,Wanhui Liu~(1,2),Youxin Li~2,Kaoxiang Sun~(1,2) 1 School of Pharmacy,Yantai University,30 Qingquan road,Yantai,264005,China.2State Key Laboratory of Long-acting and Targeting Drug Delivery System,Luye Pharmaceutical Co.Ltd,9 Baoyuan Road,Yantai,264003,China

In this work we report the effect of poly(amidomine)(PAMAM)dendrimers(G3,G4,G5,G3.5,G4.5)on corneal epithelium cellular uptake and transepithelial transport of puerarin as a model drug with immortalized human corneal epithelial(HCE)cell line. In addition,the G4 PAMAM dendrimer across HCE cells was investigated by flow-cytometry(FCM)and confocal laser scanning microscopy(CLSM).Cationic PAMAM dendrimers(G3,G4,G5)could significantly increase the uptake and transport of puerarin on HCE *** and CLSM studies revealed a significant level of internalization of G4 PAMAM dendrimer in HCE cells.

关键词： Dendrimers on the transport of puerarin in human corneal epithelial cell The effect of poly amidoamine

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Mannosylated lipid nano-emulsions loaded with lycorine-oleic acid ionic complex for tumor cell-specific delivery

Mannosylated lipid nano-emulsions loaded with lycorine-oleic...

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2012年中国药物制剂大会——中国药学会药剂专业委员会年会、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： Yangming Guo,Xing Liu,Xun Sun,,Tao Gong,Zhirong Zhang Key Laboratory of Drug Targeting and Drug Delivery System,Ministry of Education,West China School of Pharmacy,Sichuan University,Chengdu

OBJECTTVE:This study was to prepare a mannosylated lycorine lipid nano-emulsion formulation(M-LYC-OA-LNEs) for the aim of achieving tumor targeting delivery of lycorine(LYC).METHOD:Lycorine-oleic acid ionic complex(LYC-OA)was made in order to increase its lipophilicity.M-LYC-OA-LNEs and uncoated lycorine-oleic acid loaded lipid nano-emulsions (LYC-OA-LNEs)were prepared by solvent injection method and characterized by transmission electron microscopy(TEM),particle size,polydispersity index,zeta-potential and entrapment efficiency *** in vitro cellular uptake and cytotoxicity studies were performed on A549 cell ***:The entrapment efficiency of M-LYC-OA-LNEs was 82.7±1.6%.The cellular uptake study showed that coated LNEs were preferably taken up by A549 cells than uncoated *** effective test by MTT assay showed higher toxicity of M-LYC-OA-LNEs on A549 cell lines when compared with LYC-OA-LNEs and blank LNEs. CONCLUSION:These results demonstrated that M-LYC-OA-LNEs could be a promising formulation for tumor targeting delivery of LYC with the potential of being applied in the diagnosis and treatment of cancer.

关键词： lycorine lipid nano-emulsion mannosylation tumor targeted delivery

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