Abstract：
:Turbidimetric or light scattering assays can be used to determine the extent of aggregation in protein formulations. Using low molecular weight urokinase (LMW-UK) as a model protein, the effect of polymeric additives on heat-induced aggregation was evaluated. Previous work has shown that under 60 degrees C heat treatment, LMW-UK initially denatures and the unfolded protein associates to form soluble aggregates. Eventually, these aggregates associate to form a precipitate. The effects of polymers on the initial aggregation phase was examined. Hydroxyethyl (heta) starch, polyethylene glycol 4000, and gelatin were found to be effective, concentration-dependent inhibitors of aggregation, whereas polyvinylpyrrolidone (PVP) and polyethylene glycol 300 were ineffective. Overall, the effect of polymeric additives on the stability of thermally-stressed LMW-UK can be accounted for by preferential exclusion of the solute from the surface of the protein.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Vrkljan M,Foster TM,Powers ME,Henkin J,Porter WR,Staack H,Carpenter JF,Manning MCdoi
10.1023/a:1018935420680subject
Has Abstractpub_date
1994-07-01 00:00:00pages
1004-8issue
7eissn
0724-8741issn
1573-904Xjournal_volume
11pub_type
杂志文章abstract：PURPOSE:To investigate the influence of nanocarrier molecular size and shape on breast duct retention in normal rats using a non-invasive optical imaging method. METHODS:Fluorescein-labeled PEG nanocarriers of different molecular weights and shapes (linear, two-arm, four-arm, and eight-arm) were intraductally administ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-012-0763-z
更新日期：2012-09-01 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：PURPOSE:Percutaneous absorption assays of molecules for pharmaceutical and cosmetology purposes are important to determine the bioavailability of new compounds, once topically applied. The current method of choice is to measure the rate of diffusion through excised human skin using a diffusion cell. This method however...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-015-1654-x
更新日期：2015-08-01 00:00:00
abstract：PURPOSE:To develop a method for drawing statistical inferences from differences between multiple experimental pair distribution function (PDF) transforms of powder X-ray diffraction (PXRD) data. METHODS:The appropriate treatment of initial PXRD error estimates using traditional error propagation algorithms was tested ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-010-0259-7
更新日期：2010-12-01 00:00:00
abstract：PURPOSE:This study aims to develop liposomal formulations containing synergistic antibiotics of colistin and ciprofloxacin for the treatment of infections caused by multidrug-resistant Pseudomonas aeruginosa. METHODS:Colistin (Col) and ciprofloxacin (Cip) were co-encapsulated in anionic liposomes by ammonium sulfate g...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-018-2464-8
更新日期：2018-08-09 00:00:00
abstract：PURPOSE:The fate of inhaled salmon calcitonin (sCT) at the respiratory epithelial barrier was studied with particular emphasis on enzymatic degradation by trypsin, chymotrypsin, and neutrophil elastase. METHODS:Degradation of sCT was assessed by HPLC in cell homogenate, supernatant and intact monolayers of human respi...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-011-0553-z
更新日期：2012-01-01 00:00:00
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 wer...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-012-0738-0
更新日期：2012-08-01 00:00:00
abstract：PURPOSE:To determine whether LHRH-receptor is expressed in Calu-3, a human bronchial epithelial cell line, and to further determine whether this receptor plays a role in the transport of deslorelin, an LHRH agonist. METHODS:Using cultured monolayers of Calu-3 grown at air-interface, the presence and localization of LH...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/b:pham.0000029294.70707.74
更新日期：2004-06-01 00:00:00
abstract：PURPOSE:The aim of this study is to extend our previous studies to investigate the TerplexDNA synthetic gene carrier system in pharmacokinetics, biodistribution, and gene expression in major organs after systemic administration. METHODS:The stability of the TerplexDNA system was analyzed in vitro with a serum incubati...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1013081710135
更新日期：2001-09-01 00:00:00
abstract：PURPOSE:To investigate influence of ion induced mesophasic transformation on pharmaceutical performance of in situ gelling system consisting of glyceryl monooleate. METHODS:The prepared system showed mesophasic transformation during its conversion from sol to gel upon controlled hydration. The process of mesophasic tr...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-013-1033-4
更新日期：2013-07-01 00:00:00
abstract：PURPOSE:1. The assessment of the role of hair follicles and sweat glands in skin resistance and percutaneous iontophoretic flux of 9-desglycinamide, 8-arginine vasopressin (DGAVP) by comparing two skin species: human stratum corneum which contained hair follicles, sweat and sebaceous glands, and shed snake skin which l...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1016243706415
更新日期：1995-10-01 00:00:00
abstract：PURPOSE:The purpose of this study was to use a replicate designed trial to assess the overall, intra- and inter-subject variabilities in pharmacokinetic parameters of CGP 33101 after oral administration of tablets relative to that of powder suspended in water, and to determine the relative proportion of the intra-subje...
journal_title：Pharmaceutical research
pub_type： 临床试验,杂志文章,随机对照试验
doi：10.1023/a:1016275402723
更新日期：1995-12-01 00:00:00
abstract：PURPOSE:This prospective study aimed to evaluate the effects of genetic polymorphisms in sulindac-related metabolizing enzyme genes including FMO3 and AOX1 on the population pharmacokinetics of sulindac in 58 pregnant women with preterm labor. METHODS:Plasma samples were collected at 1.5, 4, and 10 h after first oral ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-020-2765-6
更新日期：2020-01-28 00:00:00
abstract：PURPOSE:The discovery of nano drug delivery system has rendered a great hope for improving cancer therapy. However, there are some inevitable obstacles that constrain its development, such as the physical and biological barriers, the toxicity of carrier materials and the physiological toxicity of drugs. Here, we report...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-019-2709-1
更新日期：2019-12-10 00:00:00
abstract：PURPOSE:The prognosis for glioma patients is poor, and development of new treatments is critical. Previously, we engineered polymer-based vaccines that control GM-CSF, CpG-oligonucleotide, and tumor-lysate presentation to regulate immune cell trafficking and activation, which promoted potent immune responses against pe...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-010-0361-x
更新日期：2011-05-01 00:00:00
abstract：:A rapid quantitative, enantioselective HPLC method for the analysis of the four stereoisomers, (+) and (-) erythro and (+) and (-) threo forms, of mefloquine has been developed using a Chiralpak Ad analytical column containing amylose tris-3,5-dimethylphenyl carbonate coated on silica gel and hexane/ethanol/diethylami...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015832912774
更新日期：1992-12-01 00:00:00
abstract：PURPOSE:To develop a novel bioadhesive polymer that protects peptide drugs from luminal degradation by aminopeptidase N and to evaluate the system in vitro on porcine mucosa. METHODS:EDTA was covalently bound to chitosan in order to combine the bioadhesive properties of the polymer with the well known capacity of EDTA...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1012108118670
更新日期：1997-07-01 00:00:00
abstract：:Leucine enkephalin (YGGFL) undergoes rapid degradation in sheep nasal mucosa to yield GGFL which is further degraded to FL. The activity of the nasal mucosal homogenate against YGGFL and GGFL (t1/2 12 and 7 min) was significantly greater than that observed with a nasal wash fluid (t1/2 40 and 13 min). The effect of cy...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018946829225
更新日期：1994-12-01 00:00:00
abstract：:The effects of skin storage, skin preparation, skin pretreatment with a penetration enhancer, and skin barrier removal by adhesive tape-stripping on the concurrent cutaneous transport and metabolism of nitroglycerin (GTN) have been studied in vitro using hairless mouse skin. Storing the skin for 10 days at 4 degrees C...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015822431178
更新日期：1992-03-01 00:00:00
abstract：PURPOSE:Ultrasound can be used to release a therapeutic payload encapsulated within a perfluorocarbon (PFC) emulsion via acoustic droplet vaporization (ADV), a process whereby the PFC phase is vaporized and the agent is released. ADV-generated microbubbles have been previously used to selectively occlude blood vessels ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-010-0277-5
更新日期：2010-12-01 00:00:00
abstract：PURPOSE:This study aimed to characterize the transepithelial transport of miltefosine (HePC), the first orally effective drug against visceral leishmaniasis, across the intestinal barrier to further understand its oral absorption mechanism. MATERIALS AND METHODS:Caco-2 cell monolayers were used as an in vitro model of...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-006-9170-7
更新日期：2007-03-01 00:00:00
abstract：PURPOSE:To devise experimental and computational models to predict aqueous drug solubility. METHODS:A simple and reliable modification of the shake flask method to a small-scale format was devised, and the intrinsic solubilities of 17 structurally diverse drugs were determined. The experimental solubility data were us...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1014224900524
更新日期：2002-02-01 00:00:00
abstract：PURPOSE:The purpose of this study was to determine the existence of insulin-degrading enzyme (EC 3.4.22.11) (IDE) in rat intestinal enterocytes. METHODS:Subcellular fractionation, biochemical characterization, immunoprecipitation, and western blots were employed. RESULTS:Insulin-degrading activity was localized in th...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1016263926946
更新日期：1995-08-01 00:00:00
abstract：PURPOSE:The aim of this study was to investigate the effect of hepatic or renal insufficiency on the pharmacokinetics of paclitaxel in rats. METHODS:Rats were treated with carbon tetrachloride (CCl4; 0.5 ml/kg) to induce hepatic failure or were subjected to 5/6 nephrectomy (5/6 Nx) to induce renal failure. Paclitaxel ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-004-1190-6
更新日期：2005-02-01 00:00:00
abstract：PURPOSE:Herein we report the discovery of a group of derivatized alpha-amino acids that increase the oral bioavailability of sodium cromolyn. METHODS:We prepared three N-acylated alpha-amino acids and used these compounds to demonstrate the oral delivery of cromolyn in an in vivo rat model. In vitro experiments, inclu...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1016034913181
更新日期：1996-02-01 00:00:00
abstract：PURPOSE:To investigate if gamma-Hydroxybutyrate (GHB) tolerance is mediated by alterations in GHB systemic pharmacokinetics, transport (blood brain barrier (BBB) and neuronal) or membrane fluidity. MATERIALS AND METHODS:GHB tolerance in rats was attained by repeated GHB administration (5.31 mmol/kg, s.c., QD for 5 day...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-006-9066-6
更新日期：2006-09-01 00:00:00
abstract：PURPOSE:Cisplatin, is recognized as a first line therapeutic for the treatment of non-small cell lung cancer (NSCLC). Cisplatin resistance is identified as the most detrimental complication during treatment and has been associated with upregulation of several genes, such as the anti-apoptotic gene survivin. In this stu...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-016-2016-z
更新日期：2016-12-01 00:00:00
abstract：PURPOSE:The objective of the current study was to investigate whether blood-brain barrier (BBB) permeability studies in vitro could be accelerated by running several compounds together in the same experiment. METHODS:To address this question, we compared the transport of six compounds run separately with the results o...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/b:pham.0000026424.78528.11
更新日期：2004-05-01 00:00:00
abstract：PURPOSE:Desmopressin acetate (DDAVP) is used parenterally and intranasally in the control of several diseases. Oral administration of DDAVP, while most desirable, is not practical presently due to low bioavailability. The objective of the present study was to explore the feasibility for employing oil-in-water MucoAdhes...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1016023111248
更新日期：1996-07-01 00:00:00
abstract：PURPOSE:To investigate the ability of various polymers to inhibit the crystallization of amorphous felodipine from amorphous molecular dispersions in the presence of absorbed moisture. METHODS:Spin coated films of felodipine with poly(vinylpyrrolidone) (PVP), hydroxypropylmethylcellulose acetate succinate (HPMCAS) and...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-007-9331-3
更新日期：2008-04-01 00:00:00
