Abstract:
:As a percutaneous sustained-release preparation, insulin micropiles (MPs) were prepared with biodegradable polymers poly(lactic acid) (PLA), poly(ϵ-caprolactone) (PCL) and poly(lactic-co-glycolic acid) (PLGA) as the base. The obtained PLA, PCL, and PLGA MPs of which the insulin:polymer ratio was 1:2 were administered to rat skin at 40 IU/kg and hypoglycemic effects measured for 6 days. The order of the hypoglycemic effect was PLA>PCL>PLGA. PLA MP showed the strongest hypoglycemic effect (2 days). The hypoglycemic effect of insulin PLA MP was dependent on the formulation; the order was insulin:PLA (2:1)>insulin:PLA (1:1)>insulin:PLA (1:2). As the ratio of insulin to the polymer base increased, the hypoglycemic effect increased. The area above the plasma glucose levels vs. time curves for 6 days from insulin:PLA (2:1) MPs, 10, 20, 30, and 40 IU/ kg, were 249 ± 108, 2003 ± 379, 3960 ± 794, and 6311 ± 726%·h. A dose-dependent hypoglycemic effect was obtained at 10-40 IU/kg and pharmacological availabilities were 11.1%, 44.5%, 58.6%, and 70%, respectively. Insulin:PLA (2:1) MP showed high plasma insulin level, 86.9-134.7 IU/mL, for 3 days. There was no damage to rat skin. These results suggest the usefulness of insulin:PLA (2:1) MP as a sustained-release percutaneous delivery system for insulin.
journal_name
J Drug Targetjournal_title
Journal of drug targetingauthors
Fukushima K,Ito Y,Ishihata M,Sugioka N,Takada Kdoi
10.3109/1061186X.2010.492521subject
Has Abstractpub_date
2011-04-01 00:00:00pages
212-8issue
3eissn
1061-186Xissn
1029-2330journal_volume
19pub_type
杂志文章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::Drug systems targeting tumor cells using basic fibroblast growth factor (bFGF) have been widely reported. In this study, the peptide KRTGQYKLC (bFGFp), containing cysteine at the carboxyl termination of the bFGF-derived peptide, was applied as a novel ligand targeting tumor cells. bFGFp was conjugated with bovine seru...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/10611860600849498
更新日期:2006-09-01 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::Gene augmentation has been the paradigm in the majority of gene therapy protocols but in recent years the potential of repairing the mutated gene in situ by targeted gene correction has become a reality. In fact, targeted gene repair has many advantages over conventional replacement strategies, notably the possibility...
journal_title:Journal of drug targeting
pub_type: 杂志文章,评审
doi:10.1080/10611860290016739
更新日期:2002-03-01 00:00:00
abstract::The effects of concentration, amperage and duration on the antidiuretic response induced by iontophoretic delivery of desmopressin acetate (DDAVP) were examined using a diabetes insipidus model in rats. A higher current density brought about a larger and longer antidiuretic response. Prolonged iontophoretic duration c...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/10611869509015918
更新日期:1995-01-01 00:00:00
abstract::To design a novel cytospecific photosensitizer for photodynamic antitumor therapy, a fullerene (C(60)) was chemically modified with pullulan which is a water-soluble polysaccharide with a high affinity for asialoglycoprotein receptors. Ethylene diamine was introduced to the terminal aldehyde groups of pullulan by the ...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/10611861003599479
更新日期:2010-09-01 00:00:00
abstract::Oleanolic acid (OA) is a pentacyclic triterpenoid found in various plant species. Triterpenoid compounds have been shown to inhibit tumor proliferation and to induce apoptosis in cancer cells. We synthesized an OA derivative and evaluated its inhibitory effects on cell proliferation in human colon cancer. Radioisotope...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/1061186X.2013.851684
更新日期:2014-10-07 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::A novel concept in drug delivery discussed here, takes advantage of certain properties of the drug "containers" cyclodextrins and liposomes to combine them into a single system thus circumventing problems associated with both systems. The concept, entailing entrapment of water-soluble cyclodextrin-drug inclusion compl...
journal_title:Journal of drug targeting
pub_type: 杂志文章,评审
doi:10.3109/10611869408996821
更新日期:1994-01-01 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:OBJECTIVE:Histone deacetylases (HDACs) have been revealed to be involved in cerebrovascular diseases, while the role of HDAC9 in intracranial aneurysm (IA) remains seldom studied. We aim to explore the role of the HDAC9/microRNA-92a (miR-92a)/Bcl-2-like protein 11 (BCL2L11) axis in IA progression. METHODS:Expression o...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/1061186X.2021.1878365
更新日期:2021-01-22 00:00:00
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::Sulpiride (SUL), anti-dopaminergic drug, has a specific site for absorption located in the upper portion of the gastrointestinal tract hence, its oral delivery represents a challenge regarding SUL absorption and bioavailability. So, a gastro-retentive oral platform of SUL was developed to increase its gastric residenc...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/1061186X.2019.1663526
更新日期:2020-04-01 00:00:00
abstract::Acyclovir is an antiviral agent and it has been particularly used for the treatment of herpes simplex infections. The treatment of infection in the oral cavity is often difficult, because of insufficient drug concentration in saliva when acyclovir is administered via the oral route in conventional tablet form for syst...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/10611860600566548
更新日期:2006-01-01 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::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::Intravenous targeting of anticancer agents should improve both efficacy and therapeutic index. However, rational design of targeting constructs requires detailed definition of receptor targets and must take account of polarised tissue architecture that may restrict access to chosen receptors from the bloodstream. Bact...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/10611860701195510
更新日期:2007-05-01 00:00:00
abstract::Gene delivery systems face the problem not only of the route toward the cell and tissues in question, but also of the molecularly crowded environment of both the cytoplasm and the nucleus itself. One of the physical barriers in the cytoplasm for diffusing nanoparticles is an actin network. Here, we describe the findin...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/1061186X.2010.521159
更新日期:2010-12-01 00:00:00
abstract::Polyethylene glycol-modified GoldMag nanoparticles (PGMNs) were synthesized and characterized by several analysis including transmission electron microscopy, dynamic light scattering, Fourier transform infrared spectroscopy, and vibrating sample magnetometer. Here, we showed that the composite nanoparticles have a sat...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/10611861003801842
更新日期:2011-04-01 00:00:00
abstract::Light-induced drug release has been explored as a strategy for externally modulating the release of drug from delivery systems. This study reports the development of a solid lipid nanoparticulate system (SLN) for paclitaxel (PTX), where photosensitizer-mediated oxidation of lipids was used as a mechanism for controlli...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/1061186X.2019.1571066
更新日期:2019-11-01 00:00:00
abstract::It is well established that overproduction and accumulation of the β-amyloid (Aβ) peptide 1-42 (Aβ(1-42)) is a trigger of the pathological cascade in Alzheimer's disease (AD) that manifests as cognitive impairment. Ginsenoside Rg3 is an important constituent of ginseng, plays an essential role in memory and improved c...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/1061186X.2017.1354002
更新日期:2018-02-01 00:00:00
abstract::The transport of 125I-radiolabelled latex nanoparticles across the nasal mucosa of rats was studied using a range of particle sizes and surface coatings. Translocation of the particles into the blood stream was examined by means of monitoring the radiolabel associated with the particles. Particles were detected in the...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/10611860108997935
更新日期:2001-01-01 00:00:00
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...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/1061186X.2013.879386
更新日期:2014-06-01 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::Previous studies indicated the potential of zinc protoporphyrin (ZnPP) as an antitumor agent targeting to the tumor survival factor heme oxygenase-1, and/or for photodynamic therapy (PDT). In this study, to achieve tumor-targeted delivery, styrene-maleic acid-copolymer conjugated ZnPP (SMA-ZnPP) was synthesized via am...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/1061186X.2015.1077851
更新日期:2016-01-01 00:00:00
abstract::Metal nanoparticles (NPs) may have the potential to overcome problems related to conventional chemotherapy. Metal NPs reported to play a beneficial and powerful role in cancer therapy providing better targeting, gene silencing and drug delivery. Functionalised metal NPs with targeting ligands offer a better control of...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/1061186X.2017.1400553
更新日期:2018-09-01 00:00:00
abstract::Notch pathway was found to be activated in most glioblastomas (GBMs), underlining the importance of Notch in formation and recurrence of GBM. In this study, a Notch inhibitory peptide, dominant negative MAML (dnMAML), was conjugated to elastin-like polypeptide (ELP) for tumor targeted delivery. ELP is a thermally resp...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.1080/1061186X.2017.1289537
更新日期:2017-07-01 00:00:00
abstract::In order to facilitate the intracellular delivery of macromolecules, Pep-1 peptide-modified liposomal (Pep1-Lipo) nanocarriers were designed and examined for their in vitro cell translocation capability. Pep-1 peptides were coupled via thiol-maleimide linkage to small unilamellar vesicles composed of phosphatidylcholi...
journal_title:Journal of drug targeting
pub_type: 杂志文章
doi:10.3109/1061186X.2010.511226
更新日期:2011-08-01 00:00:00
abstract::siRNA therapeutics has developed rapidly and already there are clinical trials ongoing or planned; however, the delivery of siRNA into cells, tissues or organs remains to be a major obstacle. Lipid-based vectors hold the most promising position among non-viral vectors, as they have a similar structure to cell or organ...
journal_title:Journal of drug targeting
pub_type: 杂志文章,评审
doi:10.3109/1061186X.2012.719232
更新日期:2012-11-01 00:00:00