Abstract：
:A method of immobilizing urokinase on albumin microspheres has been developed. Laser scattering, which was used to follow particle size from the initial emulsification stage to the final aqueous resuspension of the microsphere stage, showed that particle coalescence and crosslinking were critical parameters in manufacturing the microspheres. Chemical dehydration with 2,2-dimethoxypropane was used to convert an albumin emulsion into an albumin suspension and to reduce coalescence. An optimal amount of dehydrant produced 0.3-micron particles which resisted a 50 degrees C temperature challenge. Since oil/glutaraldehyde emulsion resulted in large particles with no urokinase activity, the cross-linking concentration of glutaraldehyde was reduced by solubilizing 25% (w/v) glutaraldehyde in the oil phase with n-propanol. A concentration of 0.015% (v/v) glutaraldehyde effectively immobilized urokinase and stabilized albumin microspheres. Amidolytic activity using the specific chromogenic substrate for urokinase, S-2444, showed that enzyme activity could be retained during this glutaraldehyde cross-linking.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Bhargava K,Ando HYdoi
10.1023/a:1015855622459subject
Has Abstractpub_date
1992-06-01 00:00:00pages
776-81issue
6eissn
0724-8741issn
1573-904Xjournal_volume
9pub_type
杂志文章abstract：PURPOSE:To demonstrate that polyanhydride copolymer chemistry affects the uptake and intracellular compartmentalization of nanospheres by THP-1 human monocytic cells. METHODS:Polyanhydride nanospheres were prepared by an anti-solvent nanoprecipitation technique. Morphology and particle diameter were confirmed via scan...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-008-9760-7
更新日期：2009-03-01 00:00:00
abstract：:Micelle-associated epoetin is still a possible explanation for the upsurge of pure red blood cell aplasia associated with subcutaneous use of epoetin alpha in patients with chronic renal failure. ...
journal_title：Pharmaceutical research
pub_type： 评论,信件
doi：10.1007/s11095-006-9573-5
更新日期：2006-03-01 00:00:00
abstract：PURPOSE:The aim of this study was to investigate transepithelial ionic permeation via the paracellular pathway of human Caco-2 epithelial monolayers and its contribution to absorption of the base guanidine. METHODS:Confluent monolayers of Caco-2 epithelial cells were mounted in Ussing chambers and the transepithelial ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-006-9568-2
更新日期：2006-03-01 00:00:00
abstract：PURPOSE:To investigate in vitro if P-glycoprotein (P-gp) transport can differentiate between antibiotic drugs exhibiting increased active renal clearance (CL(r)) in cystic fibrosis (CF) patients (i.e., dicloxacillin, trimethoprim) and drugs that do not exhibit this phenomenon (i.e.. cefsulodin, sulfamethoxazole). METH...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015191511817
更新日期：2002-04-01 00:00:00
abstract：PURPOSE:Novel itraconazole (ITZ)-based dry powders for inhalation (DPI) were optimized for aerodynamic and dissolution properties and contained excipients that are acceptable for inhalation. METHODS:The DPI were produced by spray drying solutions. The drug content, crystallinity state, and morphological evaluation of ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-012-0779-4
更新日期：2012-10-01 00:00:00
abstract：PURPOSE:This study compared gene expression profiles in mouse lungs after administration of the cationic polymers polyethyleneimine (PEI) or chitosan alone or formulated with a luciferase reporter plasmid (PEI-pLuc, chitosan-pLuc). METHODS:The polymers and formulations were administered intratracheally to Balb/c mice ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-006-9563-7
更新日期：2006-03-01 00:00:00
abstract：PURPOSE:Tissue partitioning is an important component of drug distribution and half-life. Protein binding and lipid partitioning together determine drug distribution. METHODS:Two structure-based models to predict partitioning into microsomal membranes are presented. An orientation-based model was developed using a mem...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-016-2085-z
更新日期：2017-03-01 00:00:00
abstract：PURPOSE:Labrasol and Gelucire 44/14 are defined admixtures of acylglycerols and PEG esters which are substrates for digestive lipases. METHODS:We investigated their in vitro gastrointestinal lipolysis to understand which compounds are, after digestion, responsible for keeping poorly water-soluble drugs in solution. Th...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-009-9906-2
更新日期：2009-08-01 00:00:00
abstract：PURPOSE:Comparison of the dissociation kinetics of rapid-acting insulins lispro, aspart, glulisine and human insulin under physiologically relevant conditions. METHODS:Dissociation kinetics after dilution were monitored directly in terms of the average molecular mass using combined static and dynamic light scattering....
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-017-2233-0
更新日期：2017-11-01 00:00:00
abstract：:Liver fibrosis is a pathological condition originating from liver damage that leads to excess accumulation of extracellular matrix (ECM) proteins in the liver. Viral infection, chronic injury, local inflammatory responses and oxidative stress are the major factors contributing to the onset and progression of liver fib...
journal_title：Pharmaceutical research
pub_type： 杂志文章,评审
doi：10.1007/s11095-014-1497-x
更新日期：2015-02-01 00:00:00
abstract：PURPOSE:The blood-brain barrier (BBB) essentially restricts therapeutic drugs from entering into the brain. This study tests the hypothesis that brain endothelial cell derived exosomes can deliver anticancer drug across the BBB for the treatment of brain cancer in a zebrafish (Danio rerio) model. MATERIALS AND METHODS...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-014-1593-y
更新日期：2015-06-01 00:00:00
abstract：:Azo polymers based upon 2-hydroxyethyl methacrylate, methyl methacrylate, and methacrylic acid, and containing N,N'-bis [(methacryloyloxyethyl)oxy(carbonylamino)]azobenzene as azo aromatic agent were evaluated in vivo as coating for colon-specific drug delivery. The gastrointestinal absorption of theophylline from cap...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1016283027139
更新日期：1995-02-01 00:00:00
abstract：PURPOSE:Myricetin (MYR) flavonoid is well-recognized for its antioxidant, anti-inflammatory and anti-tumor potential. Introducing nanomedicine was the ultimate resort to solve the imperfections of this nutraceutical, namely solubility, stability and delivery issues. The study, thus, aims at developing inhalable micropa...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-020-02794-z
更新日期：2020-04-14 00:00:00
abstract：PURPOSE:To evaluate and classify the hydrolases of the primate lung. METHODS:Homologous series of aromatic, aliphatic, and choline ester substrates were assayed with the pH-stat method to obtain the Michaelis-Menten kinetic constants, Vmax and K(m), for the enzymes in pulmonary alveolar tissue with esterase activity. ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1012004911942
更新日期：1997-02-01 00:00:00
abstract：:The delivery of therapeutic nucleic acids to neurons has the potential to treat neurological disease and spinal cord injury. While select viral vectors have shown promise as gene carriers to neurons, their potential as therapeutic agents is limited by their toxicity and immunogenicity, their broad tropism, and the cos...
journal_title：Pharmaceutical research
pub_type： 杂志文章,评审
doi：10.1007/s11095-007-9439-5
更新日期：2008-05-01 00:00:00
abstract：PURPOSE:The aim of this study was to identify the dominant factors affecting the stability of nanoemulsions, using artificial neural networks (ANNs). METHODS:A nanoemulsion preparation of budesonide containing polysorbate 80, ethanol, medium chain triglycerides and saline solution was designed, and the particle size o...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-009-0004-2
更新日期：2010-01-01 00:00:00
abstract：PURPOSE:Critical steps in the subcellular processing of poly(ethylene imine)/nucleic acid complexes, especially endosomal/lysosomal escape, were visualized by using living cell confocal laser scanning microscopy (CSLM) to obtain an insight into their mechanism. METHODS:Living cell confocal microscopy was used to exami...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1014212630566
更新日期：2002-02-01 00:00:00
abstract：PURPOSE:To evaluate organic anion transporter-mediated drug-drug interaction (DDI) potential for individual active components of Danshen (Salvia miltiorrhiza) vs. combinations using in vitro and in silico approaches. METHODS:Inhibition profiles for single Danshen components and combinations were generated in stably-ex...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-014-1437-9
更新日期：2014-12-01 00:00:00
abstract：PURPOSE:Fenebrutinib (GDC-0853), a Bruton's tyrosine kinase (BTK) inhibitor was investigated in a Phase 2 clinical trial in patients with rheumatoid arthritis (RA). Our aim was to apply a model-informed drug development (MIDD) approach to examine the totality of available clinical efficacy data. METHODS:Population pha...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-019-2752-y
更新日期：2020-01-06 00:00:00
abstract：:The stability of an antibiotic formulation (clindamycin phosphate in dextrose), which is stable at room temperature, was assessed by nonisothermal kinetic analysis at elevated temperatures. A preliminary study, conducted to establish apparent rate order, verified the appropriateness of a first-order kinetic model. The...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015840320410
更新日期：1991-05-01 00:00:00
abstract：PURPOSE:To examine the theoretical/practical utility of the liver-to-blood partition coefficient (Kpuu) for predicting drug-drug interactions (DDIs), and compare the Kpuu-approach to the extended clearance concept AUCR-approach. METHODS:The Kpuu relationship was derived from first principles. Theoretical simulations i...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-020-02797-w
更新日期：2020-03-25 00:00:00
abstract：PURPOSE:Synthetic hydrogels fabricated from photopolymerization are attractive for tissue engineering for their controlled macroscopic properties, the ability to incorporate biological functionalities, and cell encapsulation. The goal of the present study was to exploit the attractive features of synthetic hydrogels to...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-008-9619-y
更新日期：2008-10-01 00:00:00
abstract：PURPOSE:This study was conducted to investigate the cause of incomplete protein release from photopolymerized poly(ethylene glycol) (PEG) hydrogels and verify the protein-protection mechanism provided by iminodiacetic acid (IDA). METHODS:The in vitro release of bovine serum albumin (BSA) from PEG hydrogels prepared un...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-005-9395-x
更新日期：2006-03-01 00:00:00
abstract：PURPOSE:To investigate the effect of polyelectrolytes on the formation and physicochemical properties of chitosan nanoparticles (CS-NPs) used for the delivery of an anticancer drug, doxorubicin (DOX). METHOD:Three DOX-loaded CS-NPs were formulated with tripolyphosphate (CS-TP/DOX NPs), dextran sulfate (CS-DS/DOX NPs),...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-013-1251-9
更新日期：2014-05-01 00:00:00
abstract：PURPOSE:To characterize temporal exposure and elimination of 5 gold/dendrimer composite nanodevices (CNDs) (5 nm positive, negative, and neutral, 11 nm negative, 22 nm positive) in mice using a physiologically based mathematical model. METHODS:400 ug of CNDs is injected intravenously to mice bearing melanoma cell line...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-012-0784-7
更新日期：2012-09-01 00:00:00
abstract：:The efficacy of topical formulations of acidic fibroblast growth factor (aFGF) in healing of full-thickness wounds has been studied in a diabetic db+/db+ mouse model. The effect of several formulation variables, dose, and application frequency was examined. It was found that wound healing in diabetic animals treated w...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018993610801
更新日期：1994-01-01 00:00:00
abstract：PURPOSE:To identify and quantify, in vitro and in vivo (in humans), the charge-carrying species during transdermal iontophoresis of lidocaine hydrochloride as a function of the concentration of drug relative to that of sodium chloride in the anodal solution. METHODS:In vitro experiments in standard diffusion cells qua...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1013370529366
更新日期：2001-12-01 00:00:00
abstract：:The interaction between several marker solutes and a polyolefin laminate polymer was studied in several solutions. Solutions studied included mixtures of sodium chloride and dextrose (at concentrations more less typical of i.v. administration solutions) and several actual i.v. products [lactated Ringer's injection, Di...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015866420836
更新日期：1991-06-01 00:00:00
abstract：PURPOSE:Levofloxacin, a quinolone antibacterial drug, is a zwitterion at physiological pH. We examined the effect of cationic and anionic drugs on renal excretion of levofloxacin by means of in vivo clearance to characterize the mechanisms of renal excretion of this drug. METHODS:In vivo clearance was studied in male ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1012111902798
更新日期：1997-04-01 00:00:00
abstract：:The intrasubject and intersubject variabilities for CGS 16617, an angiotensin converting enzyme inhibitor, were evaluated in an open-label, repeat single-dose bioavailability trial. Eight healthy male volunteers each received a 20-mg oral dose of CGS 16617 as an aqueous solution on four separate occasions. Components ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015954609527
更新日期：1989-04-01 00:00:00
