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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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Preparation of 3,5,4-trimethoxy-trans-stilbene Microemulsion and its quality evaluation

Preparation of 3,5,4-trimethoxy-trans-stilbene Microemulsion...

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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： KANG Rong-rong HAN Meng YANG Su-fang XIANG Da-xiong Department of Pharmacy the Second Xiangya Hospital of central south university Institute of clinical pharmacy of central south university

Objective:To prepare 3',5,4-trimethoxy-trans-stilbene(BTM)Microemulsion,and evaluate its ***:For the formulation development oil,surfactants and co-surfactants was selected on the basis of BTM solubility in it as well as their efficiency to provide the microemulsion *** microemulsion existence ranges were defined through the construction of the pseudo-ternary phase diagram and effect of surfactant and cosurfactant mass ratio(Smix) on the microemulsion formation was *** microemulsion formulations were prepared and the abilities of various microemulsions to deliver BTM through the skin were evaluated in vitro using modified Franz diffusion cells fitted with porcine *** which consisted of 18.75%(w/w) of Cremopher EL35,9.375%(w/w) of Transcutol Hp,3.125%%(w/w) LABRAFIL M 1944 CS and 68.75%(w/w) of distilled water showed the best permeability *** formulation was selected as the optimised *** avergae particle size of the optimised preparation was 17.55 nm and the PDI was 0.068,the appearance and stability met the ***:Solubility of BTM was improved by *** microemulsion had characteristics of small particle,and stability.

关键词： 3,5,4-trimethoxy-trans-stilbene microemusion pseudotertiary phase diagrams topical administration

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Enhanced peptide delivery for inducing apoptosis of tumor cells

Enhanced peptide delivery for inducing apoptosis of tumor ce...

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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： Jie-Lan Ma Hu Wang Jie Zhang Tao Wang Yong-Huang Luo Chang-Bai Liu Chongqing Engineering Technology Research Centre of Veterinary Drug College of Pharmaceutical SciencesSouthwest University The Institute of Molecular Biology China Three Gorges University

Cell-penetrating peptides(CPPs) are short,often hydrophilic peptides that can deliver biologically active molecules into cells and that are likely to play a key role in the development of future bio ***,the appUcation of the CPPs is limited because the transduction efficiency is often insufficient and the cellular localization is *** investigated the effects of a penetration enhancer,l,2-Benzisothiazolin-3-One(BIT),on the uptake of a synthetic fluorescent TAT and a TAT-conjugated Green fluorescent protein or the pro-apoptotic peptide KLA,and evaluated its toxicity in various cell *** results showed that pretreatment of cells with BIT significantly enhanced the penetration efficiency of TAT and the bio-activity of TAT-KLA fusion peptide(Fig.1.2).In addition,the fluorescence of the peptide conjugate was well distributed throughout the cytosol and nucleus without membrane perforation or detectable cytotoxicity at effective *** uptake of the peptides was found to be dependent on the presence of serum and independent of the incubation *** findings imply that BIT may be a novel delivery enhancer that is suitable for improving the penetration of CPPs.

关键词： Cell-penetrating peptides(CPPs) TAT BIT Apoptosis KLA peptide

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Key Technologies for Development and Industrialization of Transdermal Delivery Systems

Key Technologies for Development and Industrialization of Tr...

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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：罗华菲药物制剂国家工程研究中心经皮给药技术室

The key technologies for development and industrialization of transdermal drug delivery systems were introduced in this report with a few specific examples conducted in our laboratory,including formulation design,in vitro evaluation,animal model estab lishment and key equipment *** isolated skins from different species,such as nude mice,rat,rabbit,mini-pig and human were used to investigate the transdermal penetrating profiles of a series of drugs,including Ethinyloestradiol,Gestodene,Granisetron,Donepezil,tulobuterol,oxybutynin,tolterodine,etc.,so as to evaluate the permeability difference through different animal skins,as well as the correlation between animals and *** experimental results indicated that there existed a high similarity between isolated mini-pig skin and human skin based on the results that 1:3.5～5 of drug permeation rate in isolated mini-pin skin and nude mice skin was similar with 1:4～5 of permeation rate in isolated human skin and nude mice skin reported in literatures,providing a useful method for the in vitro evaluation of transdermal drug delivery *** key equipments were designed and manufactured for small test,pilot scale preparation and large scale manufacturing of transdermal patches based on different processing techniques,with regard to the casting,cutting and packaging process,solving the bottleneck problems of engineering and industrialization of transdermal delivery ***,15 new transdermal patch formulations have been devebped based on our technology platform,of which 2 Certificates of New Drugs,3 Drug Product Permits and 3 Clinical Trial Approvals have been obtained.

关键词： Key Technologies for Development and Industrialization of Transdermal Delivery Systems

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Preparation,Characterization,and In Vitro Evaluation of Curcumin-Niosome

Preparation,Characterization,and In Vitro Evaluation of Curc...

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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： Yingqi Xu Shengpeng Wang Yitao Wang Meiwan Chen State Key Laboratory of Quality Research in Chinese Medicine Institute of Chinese Medical SciencesUniversity of Macau

Curcumin(Cur),a natural polyphenol derived from the rhizome of Curcuma bnga,possesses a wide range of pharmacological effects including neuroprotective ***,the neuroprotective efficacy of curcumin is limited by its poor brain bioavailability due to poor absorption and rapid ***,a novel niosome system composed of nonionic surfactants including Span80,Tween80,pobxamer 188,sodium dodecyl sulfonate and Sephadex G50 was developed to address these *** resulted niosomes were uniformly round with particle size and zeta potential at84.15 ± 4.03 nm and 21.75 ± 2.05 mV,*** entrapment efficiency of curcumin in niosomes was found to be 92.3 ± 0.4%.The evaluation of in intro drug release was assessed with the method of dynamic *** assay showed that curcumin-niosome induced significantly higher cytotoxicity against PC12 cells(IC50:20 μM),as compared to free curcumin.H202-induced oxidative stress model in the PC12 cells was employed to investigate the neuroprotective effects of *** result showed that pretreatment with 1 μM curcumin-niosome for 4 h increased the percentage of cell viability by 8.5%.Therefore,niosome might be a promising drug delivery system for curcumin to be used in neuroprotective applicatioa

关键词： curcumin niosome neuroprotective effects PC12 cell

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Peroral delivery of protien and peptide drugs by nanocarriers

Peroral delivery of protien and peptide drugs by nanocarrier...

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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：黄园四川大学华西药学院

Recent advances in biotechnology and genetic engineering have made the mass production of therapeutic biomacromolecules feasible,such as protein and peptide *** oral administration is considered to be the most convenient and preferred choice for patients,these biomacromolecular drugs are susceptible to both inactivation in the harsh pH environment of gastro-intestinal tract and degradation by proteolytic ***,their highly hydrophilic character as well as large size lead to poor permeability across intestinal biological *** is considered to be a promising vehicle for oral delivery of protein and peptide *** can offer,to some extent,drug protection and increase drug absorption through the intestinal ***,one of the greatest challenges is to overcome the absorption barrier of intestinal mucosa,consisting of intestinal epithelial cells as well as mucus *** transportation of substrates(transcellular transport or paracellular transport) through epithelium is a comp heated process,which involves multiple pathways with different *** uptake of nanoparticles by epithelial cells could be influenced by many factors,including the particle size,surface charge,hydrophobicity,and even their concentration Incorporation of targeting moieties on the particle surface could enhance their affinity to some specific sites of the epithelium and influence the mode of drug absorption Nanocarriers can be internalized by epithelium cells by process known as endocytosis,which comprises phagocytosis,pinocytosis,clathrin-mediated endocytosis,and nonclathrin-mediated ***,transcellular transport from the intestinal lumen to extracellular fluid may occur through *** ligands that mediate an endocytosis that not is followed by transcytosis may not be a suitable *** addition,the permeation of drugs from the intestinal lumen to the systemic circulation could also be achieved by the trans

关键词： Peroral delivery of protien and peptide drugs by nanocarriers

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Silk fibroin/gelatin electrospunnanofibrous dressing functionalized with Astragaloside Ⅳ induces healing and anti-scar effects on burn wound

Silk fibroin/gelatin electrospunnanofibrous dressing functio...

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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： Ying-Hui Shan Li-Hua Peng Xin Liu Xi Chen Ping Li Jie Xiong Jian-Qing Gao Institute of Pharmaceutics College of Pharmaceutical SciencesZhejiang University College of Materials and Textiles Zhejiang Sci-Tech University

Functbnal wound dressing has provided new challenges for researchers who focus on burn to improve skin graft quality,reduce scarring,and develop a pluristratified dermal or epidermal construct of a burn *** study aimed to investigate the effect of a silk fibroin/gelatin(SF/GT) electrospunnanofibrous dressing loaded with Astragaloside IV(AS) on deep partial-thickness burn ***-baded SF/GT-blended nanofibrous dressing was prepared by electrospinning *** optimal ratio(25:75) of silk fibroin to gelatin was further optimized by evaluating ATR-FTIR characteristics,mechanical properties,porosity,swelling rate,degradation,and release profile of the AS-baded SF/GT nanofibrous *** contrast to the blank control,the AS-baded SF/GT nanofibrous dressing promotedcell adhesbn and proliferatbn with good bbcompatibility in vitro(p< 0.01).This dressing also accelerated wound healing and inhibited scar formatbn in vivo by stimulating wound cbsure(p < 0.05),increasing angiogenesis,regulating newly formed types of collagen,and improving collagen organization These results showed that SF/GT nanofibrous dressing is a promising topical drug delivery ***,AS-functionalized SF/GT nanofibrous dressing is an excellent topical therapeutic that could be applied to promote healing and elicit anti-scar effects on partial-thickness burn wound.

关键词： burn nanofibrous dressing Astragaloside IV wound healing scar inhibition

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The Effects of Polysaccharide and Oligosaccharide from Trigonella Foenum-graecum Seeds on Dyslipidemia

The Effects of Polysaccharide and Oligosaccharide from Trigo...

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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： Chen Zhi Wang Wenping Sui Hong School of Pharmacy Ningxia Medical University Ningxia Engineering & Technology Research Center For Modernization of Hui Medicine Key Lab of Hui Ethnic Medicine Modernization Ministry of Education

Objective:To investigate the inhibitory effect of polysaccharide(PS) and oligosaccharide(OS) of Trigonella foenum-graecum seeds(TFGs) on dyslipidemia,and to preliminarily elucidate the ***:The combinative activity of PS and OS on cholesterol and bile acid was determined in *** rats were fed with high fat diet(HFD) for 3 weeks,and used as the hyperlipidemia *** rats were divided into 5 groups(control,HFD,HFEH+polysaccharide,HFD+oligosaccharide,HFD+atorvastatin respectively) and sacrificed after treated for 9 *** parameters and peroxide parameters in serum were *** assay of liver tissues were *** and bile acid in feces were also extracted and ***:Compared with the HFD group,total cholesterol(TC),triglyceride(TG),low density lipoprotein(LDL),high density lipoprotein(HDL) level,and liver tissues histopathologic slices of each treated group were significantly improved,without elevating the aspartate amino transferase(AST) and alanine amino transferase(ALT)*** and OS exhibited capacity of modulating the dyslipidemia with no obvious hepatic *** superoxide dismutase(SOD) level of PS and OS group were suppressed,and significant lower mabndiaklehyde(MDA) level was found in OS group.3-hydroxy-3-methyl-glutaryl-CoA reductase(HMG-CoAR) level was lowered in all treated ***,an up-regulate tendency of excretion of the bile acid,which is considered to be the metabolite of cholesterol,was observed in PS and OS ***:Polysaccharide and oligosaccharide of TFGs Showed considerable remedy effects on dyslipidemia,which probably relate to the cholesterol-bile acid dynamic equilibrium.

关键词： TFGs polysaccharide oligosaccharide lipid-lowering cholesterol-bile acid dynamic equilibrium

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Preparation,Characterization and evaluation of Antitumor Effect of Brucea Javanica Oil Cationic Nanoemulsion

Preparation,Characterization and evaluation of Antitumor Eff...

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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： Wei Dai De-Hua Liao Rong-Rong Kang Xiong-Bin Hu Li-Qiu Mu Tian-Qian Tang Xin-Yi Liu Da-Xiong Xiang Department of Pharmacy the Second Xiangya Hospital of central south university Institute of clinical pharmacyof central south university

The main purpose of the present study was to prepare Brucea Javanica Oil Cationic nanoemulsion(BJO-CN) for oral administration and evaluate the anti-tumor *** antitumor effect of BJO-CN was studied by developing the subcutaneous xenograft model in nude mouse of human pulmonary adenocarcinoma cell *** relative tumor volume(RTV),the rate of relative tumor volume(T/C(%) as well as the tumor volume doubling time(TVDT) between BJO-OE(Brucea Javanica Oil Oral Emulsion sold in the market) group and 1/2BJO-CN group had no statistical *** T/C(%) of BJO-OE group and 1/2BJO-CN group were 48.6%and 49.2%*** TVDT of BJO-OE group and 1/2BJO-CN group were 15.3 days and15.0 days ***,the effect of BJO-OE group and 1/2 BJO-BN group to up-regulate or down-regulate the expression of proteins(VEGF,caspase-3 and p53)was *** conclusion,BJO-CN could improve the inhibitbn to the growth of xenograft of BJO,and decrease the oral drug *** absorption mechanism was mainly induced by the positively charged droplets connected with the negative charge sites in the gastrointestinal mucosa,via mainly by electrostatic and muco-adhensive approaches to promote the absorption of BJO-CN.

关键词： Preparation,Characterization and evaluation of Antitumor Effect of Brucea Javanica Oil Cationic Nanoemulsion

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Dual targeting for metastatic breast cancer and tumor neovasculature by EphA2-mediated nanocarriers

Dual targeting for metastatic breast cancer and tumor neovas...

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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： Zhaoming Guo Bing He Lan Yuan Qiang Zhang Skate Key Laboratory of Natural and Biomimetic Drugs School of Pharmaceutical SciencesPeking University

EphA2 is a transmembrane receptor tyrosine kinase that is highly expressed on both tumor neovascukture and some kinds of tumor ***,a homing peptide with a sequence of YSAYPDSVPMMSK(YSA) that binds specifically with EphA2 was utilized to modify the stealth liposomes(YSA-LP).With a particle size of about 85 nm,this functionalized nanocarrier was loaded with fluorescent probe or doxorubicin(DOX) and investigated in vitro and in *** the cellular endocytosis studies in vitro,coumarin-6 baded YSA-LP exhibited significant specificity to both EphA2-overexpressing tumor cells(MDA-MB-231) and human umbilical vein endothelial cells(HUVEC) vk a YSA mediated interaction In a MDA-MB-231 xenograft tumor mouse model,DiR-loaded YSA-LP showed more lasting accumulatbn in tumor tissue by small animal imaging compared to unmodified liposomes(LP).Further,YSA-LP greatly facilitated the efficacy of DOX baded against both tumor cells and tumor angbgenesis in the same mouse model,evidenced by inhibiting tumor growth,metastasis and CD31 expressbn as well as inducing cancer cell ***,YSA-LP(DOX) showed rektively low systemic and cardiac toxicity compared with control *** conclusbn,YSA might be a promising targeting motif for EphA2-overexpressing tumor cells and tumor neovascukture,which could be used to medkte drug dehvery for chemotherapy agents.

关键词： Tumor neovasculature tumor cells liposome targeted delivery metastatic breast cancer

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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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