Abstract：
PURPOSE:We compared cationic, polyamine-coated microparticles (MPs) and anionic, protein-coated MPs with respect to their phagocytosis and phagosomal fate in dendritic cells (DCs) and macrophages (Mphi). METHODS:Polystyrene MPs were surface modified by covalent coupling with fluorescein isothiocyanate-labeled polyamines or proteins. Phagocytosis of MP and the pH of their intracellular microenvironment was assessed in human-derived DCs and Mphi in a fluorescence plate reader. Visualization of MP phagocytosis in DCs was performed by transmission electron microscopy. RESULTS:Phagocytosis of bovine serum albumin-coated MPs was low with significant differences between DC and Mphi, whereas phagocytosis of IgG-coated MPs was significantly enhanced in both cell types. Phagocytosis of both particle types resulted in an acidified phagosomal microenvironment (pH 4.6-5.1). In contrast, cationic, polyamine-coated MPs were equally phagocytosed by DCs and Mphi to a high extent and showed lower degrees of acidification (pH 6.0-6.8) in the phagosomal microenvironment. Transmission electron microscopy examination demonstrated all phagocytosed particles to be surrounded by a phagosomal membrane, which was more tightly apposed to the surface of cationic MPs and more loosely to bovine serum albumin-coated MPs. CONCLUSION:Phagocytosis of cationic, polyamine-coated MPs is suggested to lead to diminished phagosomal acidification. Thus, cationic MP are potential carriers that may display beneficial features for the intracellular delivery of immunomodulating therapeutics and their protection against lysosomal degradation.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Thiele L,Merkle HP,Walter Edoi
10.1023/a:1022271020390subject
Has Abstractpub_date
2003-02-01 00:00:00pages
221-8issue
2eissn
0724-8741issn
1573-904Xjournal_volume
20pub_type
杂志文章abstract：PURPOSE:The objective of this study was to compare two different nebulizers: Eflow rapid® and Pari LC star® by scintigraphy and PK modeling to simulate epithelial lining fluid concentrations from measured plasma concentrations, after nebulization of CMS in baboons. METHODS:Three baboons received CMS by IV infusion and...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-015-1716-0
更新日期：2015-10-01 00:00:00
abstract：PURPOSE:The aim of the study was to evaluate organogel nanoparticles as a lipophilic vehicle to increase the oral bioavailability of poorly soluble compounds. Efavirenz (EFV), a Biopharmaceutical Classification System (BCS) Class II, was used as drug model. METHODS:Organogel nanoparticles loaded with EFV were formulat...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-020-02808-w
更新日期：2020-05-11 00:00:00
abstract：PURPOSE:Relatively large (>5 microm) and porous (mass density <0.4 g/cm3) particles present advantages for the delivery of drugs to the lungs, e.g., excellent aerosolization properties. The aim of this study was, first, to formulate such particles with excipients that are either FDA-approved for inhalation or endogenou...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018910200420
更新日期：1999-11-01 00:00:00
abstract：PURPOSE:To test the hypothesis of surface displacement as the underlying mechanism for IgG stabilization by polysorbates and HPβCD against surface-induced aggregation. METHODS:Adsorption/desorption-kinetics of IgG-polysorbate 80/-HPβCD were monitored. Maximum bubble pressure method was used for processes within second...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-012-0854-x
更新日期：2013-01-01 00:00:00
abstract：PURPOSE:To examine the iontophoretic delivery of ALA as a function of pH and to determine the principal mechanisms responsible for its electrotransport. METHODS:Anodal iontophoretic transport of ALA was measured as a function of its concentration and pH of the donor solution. Experiments were performed in vitro using ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1011050829531
更新日期：2001-03-01 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:Using human lung cancer cells, we evaluated the involvement of plasminogen activator inhibitor-1 (PAI-1) in the anti-invasive action of cannabidiol, a non-psychoactive cannabinoid. METHODS:Invasion was quantified by a modified Boyden chamber assay. PAI-1 protein in cell culture media and PAI-1 mRNA were determ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-010-0219-2
更新日期：2010-10-01 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:To produce and characterize a nonviral ultrasound-controlled release system of plasmid DNA (pDNA) encapsulated in gas-filled poly(D,L-lactide-co-glycolide) microparticles (PLGA-MPs). METHODS:Different cationic polymers were used to form pDNA/polymer complexes to enhance the stability of pDNA during micropartic...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1014430631844
更新日期：2002-03-01 00:00:00
abstract：PURPOSE:This study seeks to develop fiber membranes for local sustained delivery of 25-hydroxyvitamin D3 to induce the expression and secretion of LL-37 at or near the surgical site, which provides a novel therapeutic approach to minimize the risk of infections. METHODS:25-hydroxyvitamin D3 loaded poly(L-lactide) (PLA...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-015-1667-5
更新日期：2015-09-01 00:00:00
abstract：PURPOSE:This work explores the distribution of water and its effects on molecular mobilities in poly(vinylpyrrolidone) (PVP) glasses using molecular dynamics (MD) simulation technology. METHODS:PVP glasses containing 0.5% and 10% w/w water and a small amount of ammonia and Phe-Asn-Gly were generated. Physical aging pr...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-005-5277-5
更新日期：2005-08-01 00:00:00
abstract：:The synthesis of an homologous series of new water-soluble derivatives of pilocarpine is described. The new compounds, referred to as soft quaternary salts, are water soluble by virtue of a cationic ammonium head and their lipophilicity can be modulated by manipulating the size and the nature of the substituent in the...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015847103862
更新日期：1992-03-01 00:00:00
abstract：PURPOSE:To study the influence of solid form on the behavior of the salt siramesine hydrochloride in aqueous environments. METHODS:The solubilities and dissolution rates of siramesine hydrochloride anhydrate and monohydrate were determined at pH 3.4 and 6.4, and precipitates were examined by X-ray powder diffraction. ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-008-9783-0
更新日期：2009-04-01 00:00:00
abstract：PURPOSE:This study was conducted to assess the pharmacokinetics and pharmacodynamics of 7-nitroindazole (7-NI), a selective inhibitor of neuronal nitric oxide synthase (NOS). METHODS:Male Sprague-Dawley rats were equipped with peritoneal/ venous cannulae and a microdialysis probe in the hippocampal cortex. Rats receiv...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1013042817281
更新日期：2001-11-01 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:Short linear peptides have a high potential for delivering various drugs with therapeutic potential, including nucleic acids. Recently, we have shown that the cationic amphipathic histidine-rich peptide LAH4 (KKALLALALHHLAHLALHLALALKKA) possesses high plasmid DNA delivery capacities. Since such peptides are tho...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-010-0138-2
更新日期：2010-07-01 00:00:00
abstract：PURPOSE:To assess the uridine diphosphate (UDP)-glucuronosyltransferase (UGT) isozymes involved in the glucuronidation of niflumic acid in human liver. METHODS:The glucuronidation activity of niflumic acid was determined in liver microsomes and recombinant UGT isozymes by incubation of niflumic acid with UDP-glucuroni...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-006-0250-5
更新日期：2006-07-01 00:00:00
abstract：:Prinomide tromethamine, a nonsteroidal antiinflammatory drug, was orally administered at doses of 250, 500, and 1000 mg every 12 hr for 28 days to healthy male volunteers. The pharmacokinetic behavior of prinomide and its primary plasma metabolite displayed nonlinear characteristics, while those of free prinomide and ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018916811904
更新日期：1993-01-01 00:00:00
abstract：:Various diesters of 9-[(1,3-dihydroxy-2-propoxy)-methyl]guanine (DHPG) were screened in order to identify a derivative with improved oral absorption. The solubilities and dissolution rates decreased with increasing chain length and branching of the ester group. However, the dipropionate ester showed an anomalously fas...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1016462801968
更新日期：1987-04-01 00:00:00
abstract：PURPOSE:To evaluate the reaction of a large series of pharmacologically significant 1,4-dihydropyridine (1,4-DHP) compounds with superoxide (O2.-) in dimethylsulfoxide using differential pulse voltammetry and controlled potential electrolysis. METHODS:Differential pulse voltammetry was used to track the consumption of...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1022291624933
更新日期：2003-02-01 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:β-Hydroxy-β-methylbutyrate (HMB), a nutritional supplement, elicits anabolic activity in muscle. Here we investigated the mechanism of HMB uptake in muscle cells. METHODS:Murine muscle cells (C2C12) and human mammary epithelial cells (MCF7) were used for uptake. As HMB is a monocarboxylate, focus was on monoca...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-019-2626-3
更新日期：2019-04-17 00:00:00
abstract：PURPOSE:Gastrointestinal deposition of nanoparticles was examined after oral administration to mice suffering from an experimental gastric ulcer model. Local drug delivery could reduce side effects and would be a distinct improvement compared to existing therapeutic approaches, e.g. in the local therapy of Helicobacter...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-009-9834-1
更新日期：2009-05-01 00:00:00
abstract：PURPOSE:This study addresses the effect of freezing and thawing on a therapeutic monoclonal antibody (mAb) solution and the corresponding buffer formulation. Particle formation, crystallization behaviour, morphology changes and cryo-concentration effects were studied after varying the freezing and thawing rates, buffer...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-018-2378-5
更新日期：2018-03-19 00:00:00
abstract：PURPOSE:A theory and computer programs running on Microsoft Excel for Windows for calculation of solution pH, buffer formula, and buffer capacity at a given ionic strength and temperature were developed. The theory does not limit the category of buffer components, the number of buffer components, or the number of ioniz...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1012037819211
更新日期：1997-03-01 00:00:00
abstract：:The effects of process and storage conditions of solid-state emulsions were studied. Oil-in-water emulsions may be prepared from solid state emulsions by adding an aqueous phase to the solid. Solid-state emulsions are prepared by processing an oil phase and an aqueous solution of matrix material via a solvent removal ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018983227234
更新日期：1993-07-01 00:00:00
abstract：PURPOSE:Evidence suggests that uremic toxins such as hippurate (HA), indoleacetate (IA), indoxyl sulfate (IS), and 3-carboxy-4-methyl-5-propyl-2-furanpropionate (CMPF) promote the progression of renal failure by damaging tubular cells via rat organic anion transporter 1 (rOat1) and rOat3 on the basolateral membrane of ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-005-2486-x
更新日期：2005-04-01 00:00:00
abstract：PURPOSE:The aim of the study is to determine whether a biodegradable elastomeric device that uses an osmotic pressure delivery mechanism can release different therapeutic proteins at a nearly constant rate in nanomolar concentrations with high bioactivity, given the same formulation conditions. Vascular endothelial gro...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-006-9750-6
更新日期：2006-04-01 00:00:00
abstract：PURPOSE:To determine the extent of lateral spread and stratum corneum (SC) penetration of caffeine (CAF), hydrocortisone (HC) and ibuprofen (IBU) using a novel concentric tape stripping technique. METHOD:Ethanolic solutions of CAF, HC or IBU were applied to the forearm of 8 volunteers. At various time points, 10 succe...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-012-0731-7
更新日期：2012-08-01 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
