Abstract:
PURPOSE:An octreotide-conjugated polyamidoamine (PAMAM) dendrimer was synthesized and employed as nanocarriers of methotrexate (MTX), for targeting to the somatostatin receptors over-expressed tumor cells. METHODS:PAMAM-PEG-octreotide (PPO) and PAMAM-PEG (PPG) were synthesized and characterized. The cellular uptake of fluorescein isothiocyanate (FITC)-labeled PPO (PPO-FITC) and PPG (PPG-FITC) were investigated. The cytotoxicity of MTX and MTX nanoparticles were conducted in the MCF-7 cells. Besides, the pharmacokinetics studies on MTX nanoparticles were carried out in rats. RESULTS:The structure of PPO was verified by NMR detection and the diameter was 11.05 ± 1.80 nm, with the amount of MTX encapsulated by PPO was 30 (molecule/molecule). MTX nanoparticles possessed significantly higher cytotoxicity against MCF-7 cells compared with free MTX, especially the PPO/MTX nanoparticles. Correspondingly, the PPO-FITC carrier had higher cellular uptake efficiency compared to PPG-FITC. In addition, pharmacokinetics studies showed that PPO/MTX nanoparticles increased mean residence time and bioavailability of MTX distinctly. DISCUSSION AND CONCLUSION:With further cellular uptake test of FITC-labeled carriers, the enhanced cytotoxicity of PPO/MTX nanoparticles was reasonable to ascribe to the specific receptor-mediated endocytosis induced by octreotide. The present study suggests that this PAMAM-PEG-octreotide nanocarrier opens a new path for treating cancer with higher efficacy.
journal_name
J Drug Targetjournal_title
Journal of drug targetingauthors
Peng J,Qi X,Chen Y,Ma N,Zhang Z,Xing J,Zhu X,Li Z,Wu Zdoi
10.3109/1061186X.2013.879386subject
Has Abstractpub_date
2014-06-01 00:00:00pages
428-38issue
5eissn
1061-186Xissn
1029-2330journal_volume
22pub_type
杂志文章abstract:BACKGROUND:Synthesized dl-Nordihydroguaiaretic acid (dl-NGDA or "Nordy") can inhibit the growth of malignant human tumors, especially the tumor angiogenesis. However, its liposoluble nature limits its in vivo efficacy in the hydrosoluble circulation of human. PURPOSE:We tried to use the ultrasonic microbubble as the c...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/1061186X.2016.1144058
更新日期:2016-09-01 00:00:00
abstract::Solid tumors such as breast cancer have historically provided many challenges to anti-cancer therapy. Therapeutic hurdles to drug penetration in solid tumors include heterogeneous vascular supply and high interstitial pressures within tumor tissue, particularly in necrotic zones, lower pH and presence of leaky vascula...
journal_title:Journal of drug targeting
pub_type: 杂志文章,评审
doi:10.1080/10611860600809112
更新日期:2006-06-01 00:00:00
abstract::Liposomes have been prepared loaded with DNA (plasmid encoding for the green fluorescent protein, GFP) and additionally modified with TATp and PEG, with PEG being attached to the liposome surface via both pH-sensitive hydrazone and non-pH-sensitive bonds. The pGFP-loaded liposomal preparations have been administered i...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/10611860701498203
更新日期:2007-08-01 00:00:00
abstract::The purpose of this research is to develop ligand-targeted plasmid based gene delivery systems for gene transfer to tumor endothelium. Cell adhesion assays were used to test the peptide inhibition of human endothelial cell adsorption to vitronectin-treated tissue culture plates. A series of RGD containing peptides wer...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/10611860410001724468
更新日期:2004-05-01 00:00:00
abstract::This study was designed to exploit the ability of Peyer's patch M cells to recognize antigen-antibody complexes in the targeted delivery of a model antigen for the induction of mucosal immunity. Sensitized liposomes consisted of an entrapped model antigen, ovalbumin (OVA), and coated with unrelated antigen-antibody co...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/10611869708995854
更新日期:1997-01-01 00:00:00
abstract::Therapeutic peptides are conventionally administered via subcutaneous injection. Chitosan-based nanoparticles are gaining increased attention for their ability to serve as a carrier for oral delivery of peptides and vaccination. They offered superior biocompatibiltiy, controlled drug release profile and facilitated ga...
journal_title:Journal of drug targeting
pub_type: 杂志文章,评审
doi:10.1080/1061186X.2017.1400552
更新日期:2018-08-01 00:00:00
abstract::In this study, folate receptor (FR) targeted liposome microbubbles loaded with oridonin (ORI) (F-LMB-ORI), liposome loaded with ORI (L-ORI) and liposome microbubbles loaded with ORI (LMB-ORI) were prepared. In vitro release properties, cellular uptake and cytotoxicity in HepG-2 cells as well as in vivo antitumor effec...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/1061186X.2016.1200588
更新日期:2017-01-01 00:00:00
abstract:PURPOSE:To evaluate the internalization and subcellular fate of AS1411 aptamer (for glioma targeting) and TGN peptide (for blood-brain barrier targeting)-modified nanoparticles (AsTNPs), which was important for optimizing targeted delivery systems and realizing the potential toxicity to cells. METHODS:Organelles were ...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/1061186X.2014.886038
更新日期:2014-06-01 00:00:00
abstract::A new drug-targeting system for CD13(+) tumors has been developed, based on ultrasound-sensitive nanobubbles (NBs) and cell-permeable peptides (CPPs). Here, the CPP-doxorubicin conjugate (CPP-DOX) was entrapped in the asparagine-glycine-arginine (NGR) peptide modified NB (CPP-DOX/NGR-NB) and the penetration of CPP-DOX...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/1061186X.2015.1058802
更新日期:2016-01-01 00:00:00
abstract::Human epidermal growth factor receptor 2 (HER2) expression has been shown to be increased in several types of human tumours. In this study, for the imaging of HER2-related tumours, a modified RNA aptamer with HER2-specific targeting was labelled with (99m)Tc, by using hydrazino nicotinamide (HYNIC) as the chelator in ...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/1061186X.2013.839688
更新日期:2014-02-01 00:00:00
abstract::Cell-penetrating peptides (CPPs) are efficient vehicles to transport bioactive molecules into the cells. Despite numerous studies the exact mechanism by which CPPs facilitate delivery of cargo to its intracellular target is still debated. The current work presents methods that can be used for tracking CPP/pDNA complex...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/1061186X.2015.1095194
更新日期:2016-01-01 00:00:00
abstract:OBJECTIVE:The objective of this work was to examine the application of catechins-containing phospholipids-based ultrasonic microbubbles (PUM) in ultrasound-induced delivery. METHODS:Catechins-containing PUM were prepared by dissolving lyophilized PUM powder in catechins solution. Morphologic characteristics of catechi...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/10611860802475696
更新日期:2008-12-01 00:00:00
abstract:UNLABELLED:Polyethyleneimine (PEI) can be used as a DNA delivery mechanism in cell culture and in vivo. Cells can be transfected by using surface-bound PEI, as well as by PEI/DNA microparticles. In the present experiments we extended these observations by preparing microspheres with covalently attached PEI. Blends of p...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/10611860108995629
更新日期:2001-01-01 00:00:00
abstract::Radiolabelled poly(methylmethacrylate) (PMMA) nanoparticles were coated with rat serum albumin (RSA), serum and inactivated serum, to examine the influence of these blood components on the body distribution of a model colloidal drug carrier. The particles were incubated overnight at 37 degrees C either in a 1% solutio...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/10611869308998760
更新日期:1993-01-01 00:00:00
abstract::We have developed a new method to evaluate the transfer of macromolecular drugs to intrapulmonary lymph nodes in rats after intrapulmonary administration. By using this method, we observed that the transfer of fluorescein isothiocyanate dextrans (FDs) to the intrapulmonary lymph nodes was markedly higher than that to ...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/10611869509015955
更新日期:1995-01-01 00:00:00
abstract::Influenza, mainly caused by influenza virus, is becoming one of the major concerns in the world. Limitation in vaccines necessitates the urgent development of new therapeutic options against this virus. In the present study, we designed small interfering RNA (siRNA) targeting overlapping gene of PB1 and PB1-F2 gene of...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/10611860802473048
更新日期:2009-02-01 00:00:00
abstract::Cytokine inhibiting drugs are much more effective when delivered intracellularly to phagocytic cells in the microencapsulated form. Dexamethasone is a powerful inhibitor of TNF-α cytokine through inhibition of NF-κB which is a gene regulator of multiple pro-inflammatory cytokines. We have determined the effect of micr...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/1061186X.2011.561856
更新日期:2011-11-01 00:00:00
abstract::Improved delivery of macromolecular drugs to solid tumor is known as the enhanced permeability and retention (EPR) effect of macromolecular drugs and lipids. We report here that a prostaglandin I2 (PGI2) analogue induces enhancement of tumor-selective drug delivery, while it decreases tumor blood flow, in a rat tumor ...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/1061186031000086072
更新日期:2003-01-01 00:00:00
abstract::The adsorption behaviour of a tetrafunctional copolymer of poly (ethylene oxide)-poly (propylene oxide) ethylene diamine (commercially available as Poloxamine 908) and a diblock copolymer of poly (lactic acid)-poly (ethylene oxide) (PLA/PEG 2:5) onto a model colloidal drug carrier (156 nm sized polystyrene latex) is d...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/10611860500246175
更新日期:2005-09-01 00:00:00
abstract::Microparticles-adsorbed insulin and zinc insulin (PenfilN) were molded to self-dissolving micropiles (SDMPs) with chondroitin sulfate as the base for the percutaneous administration of insulin. Porous silicon dioxide (Sylysia 320, 440 and 730) and porous calcium silicate (FloriteRE) were used as microparticles. As a r...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/10611860701349794
更新日期:2007-06-01 00:00:00
abstract::The aim of this study was to evaluate the pharmacokinetics (PK), tissue distribution, and the specific drug targeting of cefpiramide sodium-loaded liposomes (CPMS-Lips) compared with cefpiramide sodium solution (CPMS-Sol) in mice. CPMS-Lips were prepared by reverse phase evaporation method. In the PK and biodistributi...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/10611861003667607
更新日期:2011-01-01 00:00:00
abstract::Paclitaxel is not effective for treatment of brain cancers because it cannot cross the blood-brain barrier (BBB) due to efflux by P-glycoprotein (P-gp). In this work, glutathione-coated poly-(lactide-co-glycolide) (PLGA) nanoparticles (NPs) of paclitaxel were developed for brain targeting for treatment of brain cancer...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/1061186X.2011.589435
更新日期:2011-11-01 00:00:00
abstract::Based on the organotropic characteristics of bile acids towards the liver and the intestine, two novel compounds of the Bamet family, containing at least one bile acid moiety bound to platinum(II), have been synthesized and their cytostatic effect compared to their ability to become accumulated in tumor cells of hepat...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/1061186021000001841
更新日期:2002-08-01 00:00:00
abstract::Recent research into the complex and varied components of rheumatoid arthritis (RA) is leading to the development of more effective targets for pharmaceutical approach than even before. Current treatment of RA frequently includes the use of nonsteroidal anti-inflammatory drugs, such as Diclofenac sodium (DFNa) in spit...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/10611860701725191
更新日期:2008-01-01 00:00:00
abstract::Archaeal ether glycerolipid vesicles (archaeosomes) efficiently deliver exogenous antigen for induction of humoral and cell-mediated immunity. Because induction of CD8 cytotoxic T cells is critical for protective vaccination against tumors, we compared the ability of various archaeosome lipid compositions to evoke a s...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/10611860410001670044
更新日期:2003-01-01 00:00:00
abstract::Developing a highly effective and lung-targeted local drug delivery carrier with low irritancy may be critical for improving treatment of lung cancer. Using soluble excipients as microspheres (MS) matrix, respirable MS embedding chitosan-coated poly(d,l-lactide-co-glycolide) nanoparticles (CNP-MS) for 2-methoxyestradi...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/1061186X.2013.878944
更新日期:2014-06-01 00:00:00
abstract::Local tissue toxicity, systemic toxicity and platinum pharmacokinetics were evaluated in 6 normal healthy beagle dogs injected subcutaneously with two formulations of a polylactide biodegradable polymer (Atrigel) system containing cisplatin. Dogs were injected 4 times at 30 day intervals at platinum dosages of 70, 105...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/10611869808997866
更新日期:1998-01-01 00:00:00
abstract::Highly lipophilic antitumor agent, palmitoyl rhizoxin (RS-1541), was incorporated into stable lipid emulsions about 100-1000nm in mean diameter consisting of triglyceride ODO and surfactant HCO-60. The pharmacokinetics of RS-1541 were studied after i.v. injection in mice, rats, rabbits, and dogs. Dog showed characteri...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/10611869808997875
更新日期:1998-01-01 00:00:00
abstract::The ultimate goal of bacterial based cancer therapy is to achieve non-toxic penetration and colonisation of the tumour microenvironment. To overcome this efficacy-limiting toxicity of anticancer immunotherapy, we have tested a therapy comprised of systemic delivery of a vascular disrupting agent to induce intratumoral...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/1061186X.2020.1850739
更新日期:2020-12-21 00:00:00
abstract::Doxorubicin (DXR) was encapsulated in long-circulating liposomes, composed of ganglioside GM1 (GM1)/distearoylphosphatidylcholine (DSPC)/cholesterol (CH) (0.13:1:1 in molar ratio) and sized to approximately 100 nm in mean diameter, with 98% entrapping efficiency by the transmembrane pH gradient method. Free DXR, DXR-D...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/10611869308996086
更新日期:1993-01-01 00:00:00