Abstract:
PURPOSE:The current study aimed to examine the pharmaceutical applications of the focused-ion-beam (FIB) in the inhalation aerosol field, particularly to particle porosity determination (i.e. percentage of particles having a porous interior). MATERIALS AND METHODS:The interior of various spray dried particles (bovine serum albumin (BSA) with different degrees of surface corrugation, mannitol, disodium cromoglycate and sodium chloride) was investigated via FIB milling at customized conditions, followed by viewing under a high resolution field-emission scanning electron microscope. Two sets of ten particles for each sample were examined. RESULTS:For the spray-dried BSA particles, a decrease in particle porosity (from 50 to 0%) was observed with increasing particle surface corrugation. Spray-dried mannitol, disodium cromoglycate and sodium chloride particles were determined to be 90-100%, 0-10% and 0% porous, respectively. The porosity in the BSA and mannitol particles thus should be considered for the aerodynamic behaviour of these particles. CONCLUSIONS:The FIB technology represents a novel approach useful for probing the interior of particles linking to the aerosol properties of the powder. Suitable milling protocols have been developed which can be adapted to study other similar particles.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Heng D,Tang P,Cairney JM,Chan HK,Cutler DJ,Salama R,Yun Jdoi
10.1007/s11095-007-9276-6subject
Has Abstractpub_date
2007-09-01 00:00:00pages
1608-17issue
9eissn
0724-8741issn
1573-904Xjournal_volume
24pub_type
杂志文章abstract:PURPOSE:Present study assessed the influence of gallate esterification on the anti-cancer activity of procyanidin B2 (B2) in androgen-dependent human prostate carcinoma LNCaP cells employing B2-3,3'-di-O-gallate (B2-G(2)), two mono-gallate esters B2-3-O-gallate (B2-3G) and B2-3'-O-gallate (B2-3'G) and the parent compou...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-009-0037-6
更新日期:2010-04-01 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:To develop novel bioactive-chylomicrons to solve oral delivery obstacles of Berberine chloride and target the lymphatic system. METHODS:Berberine-loaded bioactive-chylomicrons were prepared and underwent full in vitro characterization. Intestinal permeability was appraised via both non-everted gut sac model an...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-017-2307-z
更新日期:2018-01-05 00:00:00
abstract:PURPOSE:Using monolayers of human pancreatic adenocarcinoma cells (Panc-1) that express multidrug resistance-associated protein (MRP), the present work investigates the effects of Pluronic block copolymers on the functional activity of MRP. METHODS:The studies examined the accumulation and efflux of the MRP selective ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018873702411
更新日期:1999-03-01 00:00:00
abstract::Nucleoside transporters play a critical role in the absorption, disposition, and targeting of therapeutically used nucleosides and nucleoside analogs. This review is focused on the Na(+)-dependent, concentrative nucleoside transporters which are found in a variety of cells including renal, intestinal and hepatic epith...
journal_title:Pharmaceutical research
pub_type: 杂志文章,评审
doi:10.1023/a:1012113931332
更新日期:1997-11-01 00:00:00
abstract:PURPOSE:4-Phenylbutyrate (4-PBA) is expected to be a potential therapeutic for several neurodegenerative diseases. These activities require 4-PBA transport into the brain across the blood-brain barrier (BBB). The objective of the present study was to characterize the brain transport mechanism of 4-PBA through the BBB. ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-016-1912-6
更新日期:2016-07-01 00:00:00
abstract::The effect of γ-cyclodextrin and its four derivatives on the solubility of progesterone in phosphate buffer pH 7.4 was investigated. γ-Cyclodextrin forms a complex precipitating from solution at low cyclodextrin concentrations. No precipitation of complexes was observed with the γ-cyclodextrin derivatives. This change...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/A:1016301919928
更新日期:1985-11-01 00:00:00
abstract:PURPOSE:Study the radiolysis of solid-state metoclopramide hydrochloride at various absorbed doses. Elucidate the structure of the degradation products to gain information on the radiolysis mechanisms. METHODS:Solid-state metoclopramide samples were irradiated at several doses with gamma rays and high-energy electrons...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-006-0019-x
更新日期:2006-06-01 00:00:00
abstract:PURPOSE:Hydroxylation of the antidepressant and smoking deterrent drug bupropion is a clinically important bioactivation and elimination pathway. Bupropion hydroxylation is catalyzed selectively by cytochrome P4502B6 (CYP2B6). CYP2B6-catalyzed bupropion hydroxylation has been used as an in vitro and in vivo phenotypic ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-008-9535-1
更新日期:2008-06-01 00:00:00
abstract::The application of supercritical fluid (SF) processing in pharmaceutical research is increasing particularly in the field of particle formation for drug delivery systems. The SF processes have benefits over the existing particle formation methods in terms of improved control, flexibility and operational ease. This rev...
journal_title:Pharmaceutical research
pub_type: 杂志文章,评审
doi:10.1023/a:1011957512347
更新日期:1999-07-01 00:00:00
abstract:PURPOSE:Characterization of virosomes, in late stage preclinical development as vaccines for Respiratory Syncytial Virus (RSV), with a membrane-incorporated synthetic monophosphoryl lipid A, 3D-PHAD® adjuvant. METHODS:Virosomes were initially formed by contacting a lipid film containing 3D-PHAD® with viral membranes s...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-018-2453-y
更新日期:2018-07-03 00:00:00
abstract::The origin of the microheterogeneity of a highly purified antiinflammatory humanized monoclonal antibody prepared in mammalian cell culture has been investigated. This antibody is an IgG directed toward human CD18 (a subunit of leukocyte integrins). When the IgG preparation is subjected to isoelectric focusing, it is ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018912417607
更新日期:1993-11-01 00:00:00
abstract:PURPOSE:The aim of this study was to develop a labile sphingosine-based liposome for intramuscular gene delivery. METHODS:Sphingosine-based liposomes were formulated in a range of solutions with phosphatidylcholine, then were associated to DNA. The physico-chemical characteristics of the sphingosine/EPC liposomes and ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1019894008885
更新日期:2002-08-01 00:00:00
abstract::The internalization of a neuromodulatory adrenocorticotropic hormone (ACTH) analogue, [125I]ebiratide (H-Met(O2)-Glu[125I]His-Phe-D-Lys-Phe-NH(CH2)2NH2), was examined in cultured monolayers of bovine brain capillary endothelial cells (BCEC). HPLC analysis of the incubation solution showed that [125I]ebiratide was not ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015848531603
更新日期:1992-04-01 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: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::Penetration of various compounds through shed snake skin was measured in vitro to examine the effect of lipophilicity and molecular size of a compound on permeability through this model membrane. The permeabilities were found to be controlled by the lipophilicity and the molecular size of the permeant. The smaller and...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015902308676
更新日期:1990-12-01 00:00:00
abstract::Seven healthy, male volunteers were entered into a randomized, open crossover study of the gastrointestinal transit of two enteric-coated 500-mg naproxen tablets. Two radiolabeled tablets were given to each volunteer on two occasions separated by 7 days, once in the fasted state and once after breakfast. Radiolabeling...
journal_title:Pharmaceutical research
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1023/a:1015858829187
更新日期:1992-11-01 00:00:00
abstract:PURPOSE:Bioadhesion is an important property of biological membranes, that can be utilized in pharmaceutical and biomedical applications. In this study, we have fabricated mucoadhesive drug releasing films with bio-based, non-toxic and biodegradable polymers that do not require chemical modifications. METHODS:Nanofibr...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-018-2428-z
更新日期:2018-05-22 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:PURPOSE:A Selegiline Transdermal System (STS) is under development for indications which may not be optimally or safely treated with oral selegiline. Studies were conducted to evaluate the in vitro penetration and skin metabolism of selegiline in order to better understand the toxicological findings and the observed pl...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1012051300130
更新日期:1997-01-01 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:The specific interactions between three lectin-latex conjugates and different structures of rat intestinal mucosa have been studied ex vivo. METHODS:These systems were prepared by covalent coupling of different ligands, i.e., tomato lectin (TL), asparagus pea lectin (AL), mycoplasma gallisepticum lectin (ML), ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016405126656
更新日期:1996-11-01 00:00:00
abstract:PURPOSE:Modulation of 5-HT3 receptor in the central nervous system (CNS) is a promising approach for treatment of neuropathic pain. The goal was to evaluate the role of P-glycoprotein (Pgp) in limiting exposure of different parts of the CNS to ondansetron (5-HT3 receptor antagonist) using wild-type and genetic knockout...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-020-02929-2
更新日期:2020-09-28 00:00:00
abstract::We describe an assay for acrolein in urine, employing derivatization with m-aminophenol in the presence of ferrous sulfate solution in sulfuric acid. The derivative (7-OH quinoline; DER) and the internal standard (quinine-bisulfate; IS) were separated on a 10-micron particle, 8 mm x 10-cm C18 cartridge in conjunction ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018964401677
更新日期:1993-11-01 00:00:00
abstract:PURPOSE:Evaluate the ability of (-)-6-aminocarbovir ((-)-6AC) to improve the CNS exposure to (-)-carbovir ((-)-CBV). METHODS:Activation of (-)-6AC in vitro was assessed by incubations of rat brain tissue homogenates. The in vivo brain exposure to (-)-CBV was then examined in rats after iv infusions of either (-)-CBV (...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016229624703
更新日期:1995-06-01 00:00:00
abstract:PURPOSE:To evaluate 26 marketed oncology drugs for time-dependent inhibition (TDI) of cytochrome P450 (CYP) enzymes. Evaluate TDI-positive drugs for potential to generate reactive intermediates. Assess clinical drug-drug interaction (DDI) risk using static mechanistic models. METHODS:Human liver microsomes and CYP-spe...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-012-0724-6
更新日期:2012-07-01 00:00:00
abstract::Fibers were spun by the downward configuration of the wet spinning technique. This configuration is capable of encapsulating nonspherical and/or coarse particles. We examined encapsulation of propranolol hydrochloride and the ability of the fibers to act as a sustained-release delivery system for propranolol hydrochlo...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015982521706
更新日期:1989-12-01 00:00:00
abstract:PURPOSE:The purpose of this human intestinal perfusion study was to investigate the transport and metabolism of R/S-verapamil in the human jejunum (in vivo). METHODS:A regional single-pass perfusion of the jejunum was performed using a Loc-I-Gut perfusion tube in 12 healthy volunteers. Each perfusion lasted for 200 mi...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1011916329863
更新日期:1998-06-01 00:00:00
abstract:PURPOSE:The preparation of drug/cyclodextrin complexes is a suitable method to improve the dissolution of poor soluble drugs. The efficacy of the Controlled Particle Deposition (CPD) as a new developed method to prepare these complexes in a single stage process using supercritical carbon dioxide is therefore compared w...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-006-9177-0
更新日期:2007-03-01 00:00:00