Abstract:
PURPOSE:To engineer optimized near-infrared (NIR) active thermosensitive liposomes to potentially achieve image-guided delivery of chemotherapeutic agents. METHODS:Thermosensitive liposomes were surface-coated with either polyethylene glycol or dextran. Differential scanning calorimetry and calcein release studies were conducted to optimize liposomal release, and flow cytometry was employed to determine the in vitro macrophage uptake of liposomes. Indocyanine green (ICG) was encapsulated as the NIR dye to evaluate the in vivo biodistribution in tumor-bearing mice. RESULTS:The optimized thermosensitive liposome formulation consists of DPPC, SoyPC, and cholesterol in the 100:50:30 molar ratio. Liposomes with dextran and polyethylene glycol demonstrated similar thermal release properties; however in vitro macrophage uptake was greater with dextran. Non-invasive in vivo NIR imaging showed tumor accumulation of liposomes with both coatings, and ex vivo NIR imaging correlated well with actual ICG concentrations in various organs of healthy mice. CONCLUSIONS:The optimized thermosensitive liposome formulation demonstrated stability at 37 °C and efficient burst release at 40 and 42 °C. Dextran exhibited potential for application as a surface coating in thermosensitive liposome formulations. In vivo studies suggest that liposomal encapsulation of ICG permits reliable, real-time monitoring of liposome biodistribution through non-invasive NIR imaging.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Turner DC,Moshkelani D,Shemesh CS,Luc D,Zhang Hdoi
10.1007/s11095-012-0738-0subject
Has Abstractpub_date
2012-08-01 00:00:00pages
2092-103issue
8eissn
0724-8741issn
1573-904Xjournal_volume
29pub_type
杂志文章abstract:PURPOSE:The objective of this study was to evaluate nanoparticle uptake by the Caco-2 monolayer model in vitro. Special emphasis was placed on the localization and the quantification of the uptake of fluorescently labeled polystyrene and poly(lactic-co-glycolic acid) (PLGA) nanoparticles. METHODS:Intracellular fluores...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015393710253
更新日期:2002-05-01 00:00:00
abstract:PURPOSE:Design of intravaginal rings (IVRs) for delivery of antiretrovirals is often guided by in vitro release under sink conditions, based on the assumption that in vivo release will follow a similar release profile. METHODS:We conducted a dose-ranging study in the female reproductive tract of pigtail macaques using...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-017-2224-1
更新日期:2017-10-01 00:00:00
abstract::To clarify the mechanism by which basic drugs accumulate in the lung, the binding selectivity of drugs to different subcellular structures of the perfused rat lung was examined. Imipramine, quinine, and metoclopramide were used as examples of basic drugs. The accumulation of basic drugs was highest in the mitochondria...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016481911538
更新日期:1987-02-01 00:00:00
abstract::The relative effectiveness of two beta-cyclodextrin derivatives, i.e., dimethyl-beta-cyclodextrin (DM beta CD) and hydroxypropyl-beta-cyclodextrin (HP beta CD), in enhancing enteral absorption of insulin was evaluated in the lower jejunal/upper ileal segments of the rat by means of an in situ closed loop method. The i...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018997101542
更新日期:1994-08-01 00:00:00
abstract::The stability of a freeze-dried model protein, ribonuclease A (RNase), was investigated under accelerated storage conditions at 45 degrees C for time periods up to 60 days. Because RNase is a fairly stable molecule around pH 7, lyophilization was performed in phosphate buffers at pH 4.0 or 10.0 to accelerate degradati...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015959604616
更新日期:1990-10-01 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:This paper attempts to correlate the hydrophobic contribution constants (faa) of 21 amino acids in small peptides with commonly used physiochemical parameters. These faa constants can then be used to predict hydrophobicity change in peptides when any one of the amino acid residue is substituted with another. M...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016008102587
更新日期:1996-08-01 00:00:00
abstract:PURPOSE:This study was conducted to investigate in vivo the impact of interferon-alpha (IFN)-alpha on P-glycoprotein (P-gp) activity in rats by studying how its administration modifies the bioavailability of digoxin, a fairly pure P-gp substrate. METHODS:Human recombinant IFN-alpha was given to rats (n = 5-7 per group...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-005-7415-5
更新日期:2005-11-01 00:00:00
abstract:PURPOSE:To explore the application of scanning ion occlusion sensing (SIOS) as a novel technology for characterization of nanoparticles. METHODS:Liposomes were employed as model nanoparticles. The size distribution of the liposomes was measured by both SIOS and dynamic light scattering (DLS). Particle number concentra...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-012-0788-3
更新日期:2012-09-01 00:00:00
abstract:PURPOSE:To assess the role of intestinal CYP2D6 in oral first-pass drug clearance by comparing the enzyme content and catalytic activity of a prototype CYP2D6 substrate, metoprolol, between microsomes prepared from human intestinal mucosa and from human livers. METHODS:Microsomes were prepared from a panel of 31 human...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018989211864
更新日期:1999-08-01 00:00:00
abstract:PURPOSE:Although flomoxef (FMOX) has attracted substantial attention as an antibiotic against extended-spectrum beta-lactamase-producing Escherichia coli (ESBL-producing E. coli), the pharmacokinetics/pharmacodynamics (PK/PD) characteristics of FMOX against ESBL-producing E. coli is unclear. The aim of this study was t...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-020-02977-8
更新日期:2021-01-06 00:00:00
abstract:PURPOSE:To provide a systematic biophysical approach towards a better understanding of impact of conjugation chemistry on higher order structure and physical stability of an antibody drug conjugate (ADC). METHODS:ADC was prepared using thiol-maleimide chemistry. Physical stabilities of ADC and its parent IgG1 mAb were...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-013-1274-2
更新日期:2014-07-01 00:00:00
abstract::A procedure is described that is suitable for the radioimmunoassay (RIA) of 9-[(l,3-dihydroxy-2-propoxy)-methyl]guanine (DHPG) in plasma or serum at concentrations as low as 0.7 ng/ml (2.75 × 10(-9) M). Antiserum was prepared by coupling DHPG monohemisuccinate to bovine serum albumin and immunizing rabbits with the re...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/A:1016397520991
更新日期:1986-04-01 00:00:00
abstract:PURPOSE:The objective of the work was to evaluate the potential of hyaluronan-based nanoparticles as tumor-targeting nano-systems for CD44-overexpressed cancer therapy. METHODS:The synthesized amphiphilic cholesteryl succinoyl hyaluronan (Chol-Suc-HA) conjugates self-assembled into docetaxel(DTX)-loaded nanoparticles ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-014-1393-4
更新日期:2014-11-01 00:00:00
abstract:PURPOSE:To measure the diffusion of nanometer polymersomes through tissue engineered human oral mucosa. METHODS:In vitro models of full thickness tissue engineered oral mucosa (TEOM) were used to assess the penetration properties of two chemically different polymersomes comprising two of block copolymers, PMPC-PDPA an...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-009-9882-6
更新日期:2009-07-01 00:00:00
abstract:PURPOSE:The purpose of this study was to stabilize the vinca alkaloids, vincristine sulfate (VCR) and vinblastine sulfate (VBL), in poly(lactide-co-glycolide) (PLGA) microspheres and to release the drugs in a sustained manner for more than a month. METHODS:An oil-in-oil emulsion-solvent extraction method was used to e...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1007522013835
更新日期:2000-06-01 00:00:00
abstract:PURPOSE:To compare the systemic delivery of deslorelin following intratracheal administration of different deslorelin formulations. The formulations included dry powders of deslorelin, large-porous deslorelin-poly(lactide-co-glycolide) (PLGA) particles, and small conventional deslorelin-PLGA particles. Also, solution f...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/b:pham.0000032997.96823.88
更新日期:2004-07-01 00:00:00
abstract:PURPOSE:The purpose of the current study is to evaluate the solubility advantage offered by celecoxib (CEL) amorphous systems and to characterize and correlate the physical and thermodynamic properties of CEL and its amorphous molecular dispersions containing poly(vinylpyrrolidone) (PVP). METHODS:The measurement of cr...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/b:pham.0000045226.42859.b8
更新日期:2004-10-01 00:00:00
abstract::One thousand milligrams of aspirin, as its lysine salt was administered intravenously, orally, and intramuscularly to nine male and nine female young healthy adult volunteers. After intravenous injection mean (+/- SD) values of clearance, steady-state volume of distribution, and terminal half-life were 12.2 +/- 2.2 ml...
journal_title:Pharmaceutical research
pub_type: 临床试验,杂志文章
doi:10.1023/a:1015978104017
更新日期:1989-08-01 00:00:00
abstract::The limitations of traditional gas adsorption models for describing water vapor sorption by amorphous pharmaceutical solids are described and an alternative approach based on polymer solution theories is proposed. The approach is tested by comparing a priori predicted isotherms with literature data for the poly(vinylp...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018901325842
更新日期:1993-09-01 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:PURPOSE:Good glycaemic control is essential to minimize the risk for diabetes-induced complications. Also, compliance is likely to be higher if the procedure is simple and painless. This study was designed to validate painless intradermal delivery via a patch-like microneedle array. MATERIALS AND METHODS:Diabetes was ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-007-9256-x
更新日期:2007-07-01 00:00:00
abstract:PURPOSE:HSP90 (Heat shock protein 90kD) has been validated as a therapeutic target in Castrate Resistant Prostate Cancer. Unfortunately, HSP90 inhibitors suffer from dose-limiting toxicities that hinder their clinical applications. Previously developed polymeric delivery systems for HSP90 inhibitors had either low drug...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-017-2249-5
更新日期:2017-12-01 00:00:00
abstract::Diltiazem (DTZ) is a calcium channel blocker widely used in the treatment of angina and hypertension. DTZ undergoes extensive metabolism yielding several metabolites, some of which are active like N-desmethyldiltiazem (MA), desacetyldiltiazem (M1) and N-desmethyl,desacetyldiltiazem (M2). Due to the nature of its biotr...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016226601988
更新日期:1995-04-01 00:00:00
abstract::The pulmonary deposition and pharmacokinetics of human growth hormone (hGH), administered by aerosol and instillate, in formulations containing 99mTc-DTPA (for gamma scintigraphic imaging) have been studied in five male New Zealand White rabbits. Gamma scintigraphy indicated that the peripheral:central deposition tend...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016292232513
更新日期:1995-03-01 00:00:00
abstract:PURPOSE:The lack of effective delivery vehicles impedes in vivo applications of siRNA. The trimethyl chitosan-cysteine (TC) nanoparticles (NPs) were developed for in vivo delivery of tumor necrosis factor α (TNF-α) siRNA via oral gavage and intraperitoneal injection. METHODS:The nanoparticles formulated from TC conjug...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-013-1086-4
更新日期:2013-10-01 00:00:00
abstract:PURPOSE:To investigate the effect of benzofusion on NO donor properties and related biological activities of the furoxan system. The biological properties considered were the ability to increase the cytosolic levels of cGMP in C6 cells and vasodilation. METHODS:NO donor properties were investigated either in the prese...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018974409622
更新日期:1999-06-01 00:00:00
abstract:PURPOSE:The objective of this study was to evaluate the in vivo consequences of glycyl-glutamate coadministration on gabapentin oral absorption. METHODS:Rats were administered gabapentin (10 mg/kg plus radiotracer) by gastric gavage, in the absence and presence of dipeptides, and by intravenous administration. Serial ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-007-9272-x
更新日期:2007-08-01 00:00:00
abstract::For the last 50 years we have known of a broad-spectrum agent tilorone dihydrochloride (Tilorone). This is a small-molecule orally bioavailable drug that was originally discovered in the USA and is currently used clinically as an antiviral in Russia and the Ukraine. Over the years there have been numerous clinical and...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-020-02799-8
更新日期:2020-03-25 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