Abstract：
PURPOSE:To evaluate the potential of ascorbate as a novel ligand in the preparation of pharmaceutical nanocarriers with enhanced tumor-cell specific binding and cytotoxicity. METHODS:Palmitoyl ascorbate was incorporated into liposomes at varying concentrations. A stable formulation was selected based on size and zeta potential measurements. A co-culture of cancer cells with GFP expressing non-cancer cells was used to determine the specificity of palmitoyl ascorbate liposome binding. Liposomes were fluorescently labeled to facilitate analysis by flow cytometry and fluorescence microscopy. The cytotoxic action of palmitoyl ascorbate liposomes against a variety of cell types was assayed using a standard metabolic assay. The cytotoxic effect of a low dose of paclitaxel incorporated in palmitoyl ascorbate liposomes on various cell lines was also determined. RESULTS:Palmitoyl ascorbate liposomes associated preferentially with various cancer cells compared to non-cancer cells in a co-culture model. Palmitoyl ascorbate liposomes exhibited anti-cancer toxicity in numerous cancer cell lines. Furthermore, ascorbate liposomes enhanced the effectiveness of encapsulated paclitaxel compared to paclitaxel encapsulated in 'plain' liposomes. CONCLUSIONS:Surface modification of liposomes with ascorbate residues represents a novel way to target and kill certain types of tumor cells and additionally can potentiate the effect of paclitaxel delivered by the liposomes.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
D'Souza GG,Wang T,Rockwell K,Torchilin VPdoi
10.1007/s11095-008-9674-4subject
Has Abstractpub_date
2008-11-01 00:00:00pages
2567-72issue
11eissn
0724-8741issn
1573-904Xjournal_volume
25pub_type
杂志文章abstract：PURPOSE:This study was designed to investigate the stability of recombinant FVIII (rFVIII) in solution at different pHs and to probe the cause(s) of rFVIII inactivation under accelerated storage conditions. METHODS:Aqueous stability samples of full-length rFVIII at different pHs were incubated at 40 degrees C for seve...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1023271405005
更新日期：2003-04-01 00:00:00
abstract：PURPOSE:Since glomerular filtration rate (GFR) is responsible for the elimination of a large number of water-soluble drugs, the aim of this study was to develop a semi-physiological function for GFR maturation from neonates to adults. METHODS:In the pharmacokinetic analysis (NONMEM VI) based on data of gentamicin, tob...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-014-1361-z
更新日期：2014-10-01 00:00:00
abstract：PURPOSE:The objective of this study was to develop and evaluate a pulsatile drug delivery system based on an impermeable capsule body filled with drug and an erodible plug placed in the opening of the capsule body. METHODS:The erodible plugs were either prepared by direct compression followed by placing the tablets in...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1011940718534
更新日期：1998-03-01 00:00:00
abstract：:A novel floating controlled-release drug delivery system was formulated in an effort increase the gastric retention time of the dosage form and to control drug release. The buoyancy was attributed to air and oil entrapped in the agar gel network. A floating controlled-release 300-mg theophylline tablet having a densit...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018921830385
更新日期：1993-09-01 00:00:00
abstract：PURPOSE:The United States Pharmacopoeia (USP) imposes strict requirements on the geometry and operating conditions of the USP Dissolution Testing Apparatus II. A previously validated Computational Fluid Dynamics (CFD) approach was used here to study the hydrodynamics of USP Apparatus II when the impeller was placed at ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-007-9477-z
更新日期：2008-02-01 00:00:00
abstract：PURPOSE:Overexpression of hyaluronan (HA) receptors on cancer cells results in enhanced endocytotic uptake of the drug conjugate. An N-(2-hydroxypropyl)methacrylamide (HPMA)-HA polymeric drug delivery system was used for targeted delivery of doxorubicin to cancer cells. METHODS:HA-doxorubicin (DOX) bioconjugates (HA-D...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015170907274
更新日期：2002-04-01 00:00:00
abstract：PURPOSE:To point out the importance of heterogeneity in drug distribution processes and develop a noncompartmental approach for the description of the distribution of drug in the body. METHODS:A dichotomous branching network of vessels for the arterial tree connected to a similar venous network was used to describe th...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1016031129053
更新日期：1996-05-01 00:00:00
abstract：PURPOSE:The objective of this study was to determine the influence of the peptide bond with emphasis on the carbonyl group on the interaction with and transport by the intestinal small-peptide carrier. Therefore enalapril, a known substrate for the small-peptide carrier, has been modified to an analogue with a reduced ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018866611555
更新日期：1999-01-01 00:00:00
abstract：PURPOSE:Preparation of Nanographene oxide (NGO) - Gelatin hybrids for efficient treatment of Neuroblastoma. METHODS:Nanohybrids were prepared via non-covalent interactions. Spectroscopic tools have been used to discriminate the chemical states of NGO prior and after gelatin coating, with UV visible spectroscopy reveal...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-014-1604-z
更新日期：2015-06-01 00:00:00
abstract：PURPOSE:The aim was to investigate anticancer drug-loaded poly(carbonate-ester) nanospheres as potential drug delivery systems for cancer therapy. METHODS:Functional poly(carbonate-ester) copolymers (HPCP-SD) were synthesized by the incorporation of sulfadiazine as the tumor-targeting groups to hydroxyl groups of poly...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-010-0275-7
更新日期：2010-12-01 00:00:00
abstract：PURPOSE:To demonstrate a very effective and easy way of stabilization of amorphous indomethacin (IMC) by preparing binary mixtures with octaacetylmaltose (acMAL). In order to understand the origin of increased stability of amorphous system inter- and intramolecular interactions between IMC and acMAL were studied. METH...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-014-1385-4
更新日期：2014-10-01 00:00:00
abstract：PURPOSE:Nanocrystalline drug-polymer dispersions are of significant interest in pharmaceutical delivery. The purpose of this work is to demonstrate the applicability of methods based on two-dimensional (2D) and multinuclear solid-state NMR (SSNMR) to a novel nanocrystalline pharmaceutical dispersion of ebselen with pol...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-012-0713-9
更新日期：2012-07-01 00:00:00
abstract：PURPOSE:To evaluate micronized powder retention and detachment from inhaler surfaces following reproducible deposition by impaction, coupled with centrifugal particle detachment (CPD). METHODS:Micronized albuterol sulfate (AS) and beclomethasone dipropionate (BDP) were aerosolized as dry powders and deposited by casca...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1014451203619
更新日期：2002-03-01 00:00:00
abstract：:A quantitative analysis of the dependence of dissolution rate on the relative surface area occupied by two non-interacting drug mixtures from co-compressed slabs is described. The results from the experimental dissolution rates of each component from naproxen/phenytoin co-compressed slabs under laminar flow conditions...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018979419714
更新日期：1994-10-01 00:00:00
abstract：:RNA interference (RNAi) strategies include double-stranded RNA (dsRNA), small interfering RNA (siRNA), short hairpin RNA (shRNA), and microRNA (miRNA). As this is a highly specific technique, efforts have been made to utilize RNAi towards potential knock down of disease-causing genes in a targeted fashion. RNAi has th...
journal_title：Pharmaceutical research
pub_type： 杂志文章,评审
doi：10.1007/s11095-011-0608-1
更新日期：2011-12-01 00:00:00
abstract：PURPOSE:In this study we aimed to evaluate adaptive designs (ADs) by clinical trial simulation for a pharmacokinetic-pharmacodynamic model in oncology and to compare them with one-stage designs, i.e., when no adaptation is performed, using wrong prior parameters. METHODS:We evaluated two one-stage designs, ξ0 and ξ*, ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-015-1693-3
更新日期：2015-10-01 00:00:00
abstract：:Biotherapeutics, including recombinant or plasma-derived human proteins and antibody-based molecules, have emerged as an important class of pharmaceuticals. Aggregation and immunogenicity are among the major bottlenecks during discovery and development of biotherapeutics. Computational tools that can predict aggregati...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-011-0414-9
更新日期：2011-05-01 00:00:00
abstract：PURPOSE:Studies were conducted to evaluate whether the use of an in vitro model of the blood-brain barrier (BBB) resulted in more accurate predictions of the in vivo transport of compounds compared to the use of a human intestinal cell line (Caco-2). METHODS:The in vitro BBB model employs bovine brain capillary endoth...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1016462205267
更新日期：2002-07-01 00:00:00
abstract：PURPOSE:The objective of this investigation is to develop a rational design of Osteotropic Drug Delivery System (ODDS), which we have proposed as a novel method for drug delivery to the skeleton via bisphosphonic prodrug, based on the relationship between physicochemical and pharmacokinetic properties of bisphosphonate...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1011033326980
更新日期：2001-05-01 00:00:00
abstract：:Using brine shrimp lethality to direct fractionation, extracts of the bark of Annona bullata Rich. (Annonaceae) have yielded 16 alpha-hydroxy-(-)-kauranoic acid as a bioactive plant constituent. This previously known diterpene showed significant (ED50 8.25 x 10(-2) micrograms/ml) and selective cytotoxicity against A-5...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015819422479
更新日期：1990-04-01 00:00:00
abstract：PURPOSE:To develop a non-viral gene delivery system in the form of an oil-in-water (o/w) lipid emulsion. METHOD:Cationic lipid emulsions were formulated with soybean oil, 1,2-dioleoyl-sn-glycero-3-trimethylammonium-propane (DOTAP) as a cationic emulsifier and other co-emulsifiers. The physical characteristics of the l...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1007553106681
更新日期：2000-03-01 00:00:00
abstract：PURPOSE:To develop a streamlined strategy for pharmaceutical cocrystal preparation without knowledge of the stoichiometric ratio by preparing and characterizing the cocrystals of myricetin (MYR) with four cocrystal coformers (CCF). METHODS:An approach based on the phase solubility diagram (PSD) was used for MYR cocrys...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-014-1443-y
更新日期：2015-01-01 00:00:00
abstract：PURPOSE:The objective of this work is to understand the sequence specificity of HAV peptides and to improve their selectivity in regulating E-cadherin-E-cadherin interactions in the intercellular junctions. METHODS:Peptide 1 was modified using an alanine scanning method to give peptides 2-6. The ability of these pepti...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1011094025008
更新日期：2001-04-01 00:00:00
abstract：:The electrochemical properties of human cadaver skin were studied in a diffusion cell with impedance spectroscopy as a function of time in the absence and presence of penetration enhancers dodecyl N,N-dimethylamino acetate and Azone. An improved electrochemical model of skin is presented, and combining the novel model...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018984121415
更新日期：1993-03-01 00:00:00
abstract：PURPOSE:The objective of this work was to assess, in vitro, the passage of P-glycoprotein dependent drugs across brain capillary endothelial cells, when these drugs are associated with a reversing agent. METHODS:An in vitro model of the blood-brain barrier consisting of a coculture of brain capillary endothelial cells...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1011913723928
更新日期：1998-07-01 00:00:00
abstract：PURPOSE:To investigate plasmid DNA interactions with liposomes prepared from dimyristoylglyceroethylphosphocholine (EDMPC) and DOPE using high sensitivity differential scanning calorimetry (HSDSC). MATERIALS AND METHODS:Large unilamellar liposomes of EDMPC with DOPE (mol ratio 0-50%) were prepared. Plasmid DNA was add...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-007-9325-1
更新日期：2007-10-01 00:00:00
abstract：PURPOSE:The organic cation transporters (OCTs) and multidrug and toxin extrusions (MATEs) together are regarded as an organic cation transport system critical to the disposition and response of many organic cationic drugs. Patient response to the analgesic morphine, a characterized substrate for human OCT1, is highly v...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-018-2526-y
更新日期：2018-10-25 00:00:00
abstract：:Four lipophilic, low molecular weight drugs solubilized in phosphatidylcholine-bile salt mixed micelles were injected s.c. into the hind legs of sheep and their cumulative recoveries in lymph draining from the site of application were determined. Surprisingly, the cumulative recoveries (percentage of dose) varied betw...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015807913934
更新日期：1991-10-01 00:00:00
abstract：PURPOSE:The addition of high amounts of calcium remains a pharmaceutical concern due to its precipitation with phosphate in total parenteral nutrient (TPN) admixtures, compromising also the stability of the lipid emulsion. MATERIALS AND METHODS:Calcium-phosphate solubility was compared when using binary PN solutions v...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-008-9671-7
更新日期：2008-11-01 00:00:00
abstract：PURPOSE:In this study, a new modified nanoprecipitation approach that more efficient and simpler than conventional approach was developed to synthesize D-alpha-Tocopheryl polyethylene glycol 1000 succinate stabilized liposome-PLGA hybrid nanoparticle, loaded with simvastatin (ST-TLPN). METHODS:The optimum formulation ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-018-2485-3
更新日期：2018-08-30 00:00:00
