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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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Polysaccharide from Lentinus edodes Induced Apoptosis in H22 Tumor-Bearing Mice through Reactive Oxygen Species-Mediated MAPK Pathway

Polysaccharide from Lentinus edodes Induced Apoptosis in H22...

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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： Qi-lin Zhang Yu Zhang Kai-ping Wang Hubei Key Laboratory of Nature Medicinal Chemistry and Resource Evaluation Tongji Medical CollegeHuazhong University of Science and Technology

A water-soluble polysaccharide WEP1 purified from Lentinus edodes has been found to mainly consist of glucose with the structure of(1→3)-glucose main chains and(1→6)-glucose side chains(Fig.1).Results showed that WEP1 with a molecular weight of 538.1kDa could exhibit direct cytotoxic activity against H22 and MCF-7 cells in vitro in a dose-dependent *** antitumor effects were significantly improved with the inhibitory rates of 28.27%,35.17%and 51.72%,respectively by animal *** investigation indicated that WEP1 induced H22 cells apoptosis,including displaying typical apoptotic morphological features,such as chromatin condensation,fragmented nuclei and formation of apoptotic bodies(Fig.2).Additionally,ROS overproduction was also observed in H22 *** apoptosis induction activity was associated with increasing expression of p-JNK and suppressing p-p38 *** and MAPKs were probably targets of WEP1 in tumor suppression Subsequently,both of the two phosphorylated proteins together led to the increasing level of p53 protein,which could contribute to elevation of the ratio of Bax/Bcl-2,and then triggered to caspase-3 activation and apoptosis(Fig.3).These results indicated that antitumor and apoptosis induction activities of WEP1 might be achieved by ROS-mediated MAPK and mitochondrial apoptotic ***1 could not only be regarded as a potential therapeutic agent,but also might be a complementary agent to potentiate conventional antitumor drugs.

关键词： Polysaccharide from Lentinus edodes Induced Apoptosis in H22 Tumor-Bearing Mice through Reactive Oxygen Species-Mediated MAPK Pathway

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Improvement of dissolution rate and bioavailability of puerarin flavones by dropping pills based on self-microemulsion

Improvement of dissolution rate and bioavailability of puera...

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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： Hongbo Fan Yu Wang Guangyuan Zhang Shilin Sun Qingxiang Guan Department of Pharmacy School of PharmacyJilin University

Solid dispersion technology has been widely applied to improve the solubility and dissolution rate of poorly water-soluble drugs,owing to the formation of high-energy metastable forms of the drug in the polymer such as amorphous ***,amorphous fraction,particle size reduction and particle wettability of solid dispersion can contribute to an observed improvement of bioavailability of such hydrophobic compounds[1].In the present study,dropping pills was prepared based on self-microemulsion(DP-SM) to achieve a better dissolution rate and oral bioavailability of puerarin *** formulation of self-microemulsion and DP-SM were optimized by phase diagrams and orthogonal test *** resultant DP-SM provided 35%of drug loading and exhibited spherical structures with an average droplet size of 34.32 nm after dilutioa The dissolution rate of puerarin flavones from DP-SM was obviously increased comparing to that of dropping pills alone with 105.10%and 85.03%at 10 min *** study in rats showed that oral relative bioavailability of DP-SM was about2.36 folds against that of dropping pills *** quick dissolution rate of DP-SM led to the release of solubilised drug in self-microemulsion and the crystalline form of drug in polymer at same time,the large amount of small droplets of self-microemulsion resulted ina considerable increase of surface area and improved bioabsorption by circumventing the hepatic portal route,protecting against drug degradation in the harsh GI environment,and facilitating lymphatic transport of drugs[2].Meanwhile,amorphous solid dispersion might contribute to the improved bioavailability of drugs by increasing their saturation solubility in gastrointestinal fluids[1].It was concluded that the DP-SM might be an encouraging strategy to enhance the oral absorption of puerarin flavones.

关键词： Dropping pills self-microemulsion puerarin flavones drug dissolution oral bioavailability

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Cross-library strategy for phage display and mathematical criteria for peptide libraries

Cross-library strategy for phage display and mathematical cr...

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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： Haoran Zhang Qiang Zhang State Key Laboratory of Natural and Biomimetic Drugs School of Pharmaceutical SciencesPeking University

The key of targeting drug delivery systems lies in its targeting moieties,among which peptide ligands are most widely *** display is a technique to discover novel peptide ligands for either known purified receptors or unknown receptors on intact *** phage display scans a peptide library for ligands that can bind to a given purified *** display against intact cells(PDAIC)offers the possibility to discover peptide ligands binding to a given cell type without knowing which receptor they exactly bind *** PDAIC could create a source of functional peptide ligands to modify targeting drug delivery *** traditional phage display which always ends up with a consensual peptide sequence after 3 rounds of panning experiments,PDAIC could end up with a library of "possibly competent" peptide *** research shows sequence consensus is not a necessary characteristic of a successful panning experiment for PDAIC,but a probable characteristic of small sampling and large *** probability of Type II binding in PDAIC can be much higher than in traditional phage display,since native capsid proteins of the phage can scan a huge library of receptors on the target cell for their own *** proofs are still needed to distinguish real targeting candidates out of the possibly competent *** this research,we adopted a cross-library strategy to alleviate Type II binding and make early decisions about which sequences stand out of the possibly competent library.A commercially available phage display-12 peptide library was used and MCF7 cell was selected as the target *** carrying out three separate panning experiments,each composed of 3～4 rounds of panning following the same procedure,we obtained three possibly competent libraries.A total of 217 phage cbnes were *** overlapped sequences of the three libraries were placed more credits on and synthesized to attend further binding tests such as flow cytometry and

关键词： Cross-library strategy for phage display and mathematical criteria for peptide libraries

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Surface natures of GO navigate divergent behaviors toward macrophages

Surface natures of GO navigate divergent behaviors toward ma...

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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： NaNa Luo Wei Wei Hua Yue Guanghui Ma National Key Laboratory of Biochemical Engineering Institute of Process EngineeringChinese Academy of Sciences

Surface natures of nanoparticles(NPs) profoundly determine the interaction between *** addition to the high electrical and thermal conductivity,graphene's unique two-dimensional plane structure also endows itself with substantial attributes in biomedical application Unlike traditional zero/three dimensional nanomaterials,the nascent 2D-graphene delivered many distinguished dispositions toward *** the biological effects might not be easily defined by extrapolation of data from existing materials,which renews the call for dissection in this *** this purpose,a comprehensive biobgical profiling should be made to systematically unveil how the surface properties of the novel graphene-based nanomaterials affect their outcomes when "seen" by ***,on the base of pristine graphene,its derivative graphene oxide(GO) was synthesized with an enhanced dispersion as well as facile functionalization Inspired by the classical decorating strategies in traditional nanomaterials,we also separately modified GO's surface by polyethylene glycol(PEG),bovine serum albumin(BSA) and polyetherimide(PEI).Through building a stepwise analysis,we bore out macrophages exhibited distinguished phagocytosis and viability towards surface engineered GO *** be specific,positively charged nGO-PEI exhibited appreciable cytotoxicity towards macrophages,and then came nGO and nGO-BSA,while nGO-PEG possessed excellent *** the arrival of intracellular context,compared to nGO-BSA & nGO,nGO-PEI was more apt to interact with *** interactions disrupted mitochondria via eliciting a sharp decrease in mitochondrial membrane potential and *** it followed a fluctuation in intracellular ROS and release of Cyt c from *** translocation of Cyt c subsequently initiated the activation of caspase family and finally dictated cells into apoptosis.

关键词： Graphene Oxide Surface natures Macrophage Viability Mechanism Apoptosis

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RGD-mediated,chitosan-modified single walled carbon nanotubes for the delivery of docetaxel

RGD-mediated,chitosan-modified single walled carbon nanotube...

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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： Yue Cao Qing-Ri Cao Jing-Hao Cui College of Pharmaceutical Scicences Soochow University

Purpose:RGD-mediated,chitosan-modified single walled carbon nanotubes were designed for the tumor-targeted delivery and site specific release of *** cytotoxicity,cellular uptake,intracellular localization and cellular uptake mechanisms of nanocarriers were evaluated in vitro,and the anti-tumor effectsof nanocarriers were also studied in ***:Single walled carbon nanotubes(SWCNTs) were purified by acid oxidation(O-SWCNTs) and conjugated with docetaxel(DTX) via π-πstacking ***-loaded SWCNTs(SWCNTs-DTX) were then noncovalently functionalrzed with RGD-conjugated chitosan(CS) to prepare *** cell viability of nanocarriers was determined in A549 and MCF-7 tumor cells using the MTT *** cellular uptake and intracellular localization of RGD-CS-SWCNTs-DTX were studied,and cellular uptake mechanisms of nanocarriers were also *** anti-tumor effects of RGD-CS-SWCNTs-DTX were evaluated in A549 tumor-bearing nude ***:RGD-CS-SWCNTs-DTX was successfully designed through a series of synthesis and ***-CS-SWCNTs-DTX could significantly increase the cellular uptake and the cytotoxicity of DTX in A549 cells than MCF-7 *** microscopy images showed that RGD-CS-SWCNTs-DTX could enter the lysosome by endocytosis or penetrate through the nuclear membrane into the ***-CS-SWCNT-DTX was internalization into A549 cells through clathrin-mediated and caveolae-mediated endocytosis,while it was mainly through caveolae-mediated pathway in MCF-7 ***-CS-SWCNT-DTX significantly inhibited the growth of A549 tumor in nude ***:RGD-CS-SWCNT-DTX showed significant anti-tumor effects in vitro and in *** study provides novel nanocarriers for the tumor-targeted delivery and site specific release of anticancer drugs.

关键词： SWCNT DTX CS RGD tumor-targeted

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pH and Redox Dual Responsive Liposomes for Increased Intracellular Drug Release and Enhanced Antitumor Efficacy

pH and Redox Dual Responsive Liposomes for Increased Intrace...

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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： Xuefan Xu Can Zhang Center of Drug Discovery State Key Laboratory of Natural MedicinesChina Pharmaceutical University

To increase intracellular drug release and thus improve its anticancer efficacy,a novel2-(2-（2-carboxylcyclohexylforrnamido）-3,12-dioxy-1-（1H-imidazolyl-4-）-7,8-dithio-4,11-diazapentadecylamide-glutaric acid ditetradecanol-diester（HH-SS-E2C14） based liposome delivery system was ***-loaded liposomes（HH-SS-E2C14-L）,were fabricated by a film dispersion method and followed by an ammonium sulfate *** size of the liposomes was 135.13 ± 7.5 nm in distilled ***-SS-E2C14-L was relatively stable in physiological condition while quickly releasing doxorubicin under the stimulus of acidic pH and redox ***,the incorporation of HH-SS-E2C14 into liposomes enhanced the cellular uptake and *** IC50 of HH-SS-E2C14-L was greatly lower than that of HH-E2C14-L without disulfide bond（p < 0.05） for HepG2 hepatic carcinoma *** to the enhanced cellular uptake and elevated intracellular drug release,HH-SS-E2C14-L displayed significantly higher antitumor efficacy than that of free DOX at the dosage of 5 mg/kg in vivo（p < 0.05）.These results above indicate that HH-SS-E2C14-L could provide a promising platform to construct excellent drug delivery systems for tumor therapy.

关键词： pH and Redox Dual Responsive Liposomes for Increased Intracellular Drug Release and Enhanced Antitumor Efficacy

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Tumor microenvironment sensitive doxorubicin delivery and release to glioma using angiopep-2 decorated gold nanoparticles

Tumor microenvironment sensitive doxorubicin delivery and re...

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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： Shaobo Ruan Qin He Huile Gao Key Laboratory of Drug Targeting and Drug Delivery Systems West China School of PharmacySichuan University

Glioma,the most aggressive and common intracranial tumor,is considered as the major cause of death from central nervous systems(CNS).Although various methods have been explored to conquer it,including chemotherapy,surgical ***,it is still intractable to be treated due to its complex microenvironment and biological barrier of *** this study,a gold nanoparticle-based delivery system was *** system,An-PEG-DOX-AuNPs,was loaded with fluorescent probe of doxorubicin(DOX) through sulfydryl and hydrozone,enabling the DOX could be pH sensitively *** system was further decorated with Angiopep-2,a special ligand of low density lipoprotein receptor-related protein-1(LRP-1),which could mediate the system penetrated the blood brain barrier and target to glioma *** particle size of An-PEG-DOX-AuNPs was 39.9 nm with a zeta potential of-19.3 mV,while the DOX loading capacity was 9.7%.In vitro,the release of DOX from DOX-AuNPs was in a pH-dependent *** incubated at lower pH values,especially 5.0 and 6.0,the release ratio was much quicker than that at pH 6.8 and *** coating with PEG,the acid responsive release of DOX from PEG-DOX-AuNPs demonstrated similar behavior to that from *** uptake showed obviously higher intensity of An-PEG-DOX-AuNPs compared with ***,the interaction of both An-PEG-DOX-AuNPs and PEG-DOX-AuNPs with cell was mediated by the *** vivo,An-PEG-DOX-AuNPs could distribute into glioma at a higher intensity than that of PEG-DOX-AuNPs and free ***,the glioma bearing mice treated with An-PEG-DOX-AuNPs displayed the longest median survival time,which was 2.89-fold higher than that of *** conclusion,An-PEG-DOX-AuNPs could specifically deliver and release DOX in glioma,resulting in expanded median survival time of glioma bearing mice.

关键词： DOX AuNPs Tumor microenvironment sensitive doxorubicin delivery and release to glioma using angiopep-2 decorated gold nanoparticles

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In vitro/in vivo transdermal delivery study of NLCs loaded with the alkaloidal extract from Aconitum sinomontanum compared with SLNs

In vitro/in vivo transdermal delivery study of NLCs loaded w...

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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： Teng Guo Yong-Tai Zhang Ji-Hui Zhao Chun-Yun Zhu Nian-Ping Feng Department of Pharmaceutics School of PharmacyShanghai University of Traditional Chinese Medicine

The aims of the present study were to evaluate the rnicrostructure and study the in vitro/in vivo transdermal delivery of nanostructured Upid carriers(NLCs)loaded with alkaloid of Aconitum sinomontanum(AAS) compared with solid lipid nanoparticles(SLNs).Aqueous dispersions of NLCs were successfully prepared which had a particle size of 160.5 nm,a ZP of-24.8 mV with higher encapsulation *** formation of less ordered structures in the inner core of the particles was confirmed with X-ray diffraction and Differential scanning caforimetry *** vitro drug release of nanoparticles was significantly enhanced compared with its physical mixture and both SLNs and NLCs formulations were also less cytotoxic compared to AAS solution in HaCaT and CCC-ESF-1 ***,the coumarin-6labeled NLCs had similar biocompatibility with HaCaT and CCC-ESF-1 cells to SLNs and the cellular uptake of NLCs was strongly affected by Upid *** scanning confocal microscopy analysis exhibited the fluorochrome was primarily distributed in the cytochylema with the ***-associated transdermal fluxes of lappacontine(LA) and ranaconitine(RAN),two major effective constituents of AAS,were sUghtly higher than those achieved using *** vivo microdialysis,the AUCO-t of LA and RAN from AAS-NLCs was 3.27-fold and 4.42-fold higher than AAS-SLNs,***,stratum corneum shedding and loosing was observed in the skin of nude mouse which was covered with NLCs and SLNs and the nanoparticles with complete form may hardly penetrated the *** findings indicated that NLCs could potentially improve the transdermal delivery of the alkaloidal extract from Aconitum sinomontanum.

关键词： nanostructured lipid carriers solid lipid nanoparticles transdermal delivery cellular uptake microdialysis

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Mannosylated and Lipid A-Incorporating Cationic Liposomes Constituting Microneedle Arrays as an Effective Oral Mucosal HBV Vaccine Applicable in the ControlledTemperature Chain

Mannosylated and Lipid A-Incorporating Cationic Liposomes Co...

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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： Ting Wang Ma Xiaoyu Biao Wei Shuqin Li Ming Li Ning Wang School of Pharmacy Anhui Medical University School of Medical Engineering Hefei University of Technology

To devebp an effective,convenient and stable mucosal vaccine against hepatitis B virus（HBV）,the mannose-PEG-cholesterol/lipid A-liposomes（MLLs） loaded with HBsAg were prepared by the procedure of emulsification-lyophilization and,subsequently,filled into the microholes of microneedle array reverse molds and dried to form the proHBsAg-MLLs microneedle arrays（proHMAs）.The proHMAs were stable even at 40 ℃ for up to 3 days and hard enough to pierce porcine skin but,upon rehydration,rapidly dissolved recovering the HBsAg-MLLs without obvious changes in size and antigen association ***,immunization of mice only once with the proHMAs at oral mucosa induced robust systemic and widespread mucosal immunoresponses,as evidenced by the high levels of HBsAg-specific IgG in the sera and IgA in the sahvary,intestinal and vaginal *** addition,a strong cellular immunity against HBV had been established through a mixed Th1/Th2 response,as confirmed by a significant increase in CD8 T cells as well as the enhanced levels of IgG2 a and IFN-γ in the treated ***,the proHMAs can be conveniently vaccinated via oral mucosal route to set up a multiple immune defense against HBV invasion and,in addition,may be a stable HBV vaccine applicable in the controlled temperature chain for wide distributioa____________________

关键词： HBV Mannosylated and Lipid A-Incorporating Cationic Liposomes Constituting Microneedle Arrays as an Effective Oral Mucosal HBV Vaccine Applicable in the ControlledTemperature Chain HBsAg

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The Study of In vitro and In vivo Transdermal Properties of 8-MOP Microemusion and Its Microemulsion-based Hydrogel

The Study of In vitro and In vivo Transdermal Properties of ...

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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： Ge Ou Dehua Liao Kai Zhang Daxiong Xiang Department of Pharmacy of the Second Xiangya Hospital Institute of clinical pharmacy of central south university

Objective To Study the in vitro and in vivo transdermal properties of8-MOP microemusion and its microemulsion-based *** The 8-MOP microemusion and 8-MOP microemulsion-based hydrogel were determined using a modified Franz-type diffusion cell fitted with abdominal skin of excised anthony *** rats were used as experimental model and in vivo transdermal study of 8-MOP ME,MBH and commercially available solution were *** topical administrated preparation,blood samples were withdrawn from the fossa orbitalis of rats at predetermined time intervals,and after last bbod sampled,cut off skin.8-MOP in rat plasma and skin was determined by *** In vitro permeation studies showed that the cumulative permeation amount or permeation rate of drug between ME and MBH were not significantly different（P>0.05）.The skin residual amount of 8-MOP ME was nearly twice that of 8-MOP *** in vivo skin permeation studies showed that the AUC) values from8-MOP ME and MBH were 2.9 and 2.8 times,respectively,and were greater than the AUC（o-24） values from the commercially available 8-MOP solution The skin residual amount from ME was 4.9 times greater than the *** 8-MOP ME resulted in an increased 8-MOP skin residual amount,but the 8-MOP MBH did *** 8-MOP ME can promote the drug localization into the skin,while the8-MOP MBH can not.

关键词： 8-Methoxsalen microemulsion microemulsion-based hydrogel percutaneous administration

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