Abstract：
:A series of multilamellar liposome dispersions was prepared from lipids of soy phosphatidylcholine or hydrogenated soy phosphatidylcholine containing from 0 to 30 mol% of either cholesterol, stearylamine, or dipalmitoyl phosphatidylglycerol. The liposome dispersions were aerosolized with a Collison nebulizer for 80 min at an output flow rate of 4.7 liters of air/min. The effects of nebulization on the vesicles were determined by monitoring the release of encapsulated 5,6-carboxylfluorescein (CF) from dispersions containing approximately 200 micrograms of total CF, of which 93.1 +/- 2.4% (N = 18) was initially encapsulated. In all experiments CF was released from the liposomes while being aerosolized, and this ranged from a mean of 12.7 +/- 3.8 to 60.9 +/- 1.9% of the encapsulated CF, depending upon the lipid composition. The lipid concentration in the dispersions did not affect the rate or percentage release of CF over a range of approximately 0.5 to 50 mg per nebulized dispersion. If liposomes are to be used as drug carriers in an inhalation aerosol a lipid composition should be employed which will minimize the release of encapsulated drug caused by nebulization.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Niven RW,Schreier Hdoi
10.1023/a:1015924124180subject
Has Abstractpub_date
1990-11-01 00:00:00pages
1127-33issue
11eissn
0724-8741issn
1573-904Xjournal_volume
7pub_type
杂志文章abstract：PURPOSE:An asymmetric membrane (AM) tablet was developed for a soluble model compound to study the in vitro drug release mechanisms in challenge conditions, including osmotic gradients, concentration gradients, and under potential coating failure modes. Porous, semipermable membrane integrity may be compromised by a hi...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-006-9142-y
更新日期：2007-02-01 00:00:00
abstract：:A new method of analysis for the antihypertensive drug, hydralazine, is introduced. The assay involves the addition of p-nitrobenzaldehyde to blood samples containing hydralazine, to form a stable Schiff's base, hydralazine p-nitrobenzaldehyde hydrazone. The derivative is extracted from the blood into hexane and the s...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015915812987
更新日期：1988-06-01 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：: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:An ex vivo intact toe model was developed to assess two different applicator designs for iontophoretic delivery of terbinafine into the nail only or the nail and surrounding skin. METHODS:Iontophoretic permeation studies were carried out on intact cadaver toes using nail-only and nail/skin applicators with a c...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-009-9934-y
更新日期：2009-09-01 00:00:00
abstract：:(+)-Propranolol was infused at two rates into the pyloric vein (a portal vein tributary) of 15 male Sprague Dawley rats until apparent steady-state conditions were established (i.e., 8 hr at each rate). One group (n = 7) received the high dose (40 micrograms/min/kg) first, and in the other group (n = 8) the low dose (...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018921306200
更新日期：1994-03-01 00:00:00
abstract：PURPOSE:To characterize the distribution of water among various components in a powder blend using solid-state NMR spectroscopy. METHODS:Water sorption behavior of theophylline anhydrate and excipients was determined by dynamic vapor sorption (DVS) and Karl Fischer Titration (KFT) after storing them in humidity chambe...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-016-1972-7
更新日期：2016-10-01 00:00:00
abstract：:Inhibition of efflux pumps is an emerging approach in cancer therapy and drug delivery. Since it has been discovered that polymeric pharmaceutical excipients such as Tweens or Pluronics can inhibit efflux pumps, various other polymers have been investigated regarding their potential efflux pump inhibitory activity. Am...
journal_title：Pharmaceutical research
pub_type： 杂志文章,评审
doi：10.1007/s11095-007-9347-8
更新日期：2008-03-01 00:00:00
abstract：PURPOSE:To explain thermal stability enhancement of an organic compound, sucralose, with cyclodextrin based metal organic frameworks. METHODS:Micron and nanometer sized basic CD-MOFs were successfully synthesized by a modified vapor diffusion method and further neutralized with glacial acetic acid. Sucralose was loade...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-016-2059-1
更新日期：2017-02-01 00:00:00
abstract：PURPOSE:Our previous studies showed that the mRNA level of human organic anion transporter (hOAT) 3 in the kidney was correlated with the rate of elimination of an anionic antibiotic cefazolin. However, the correlation coefficient was not so high. In the present study, therefore, we enrolled more patients to examine wh...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-005-8383-5
更新日期：2005-12-01 00:00:00
abstract：PURPOSE:The objective of this study was to investigate the possible influence of probenecid on morphine transport across the blood-brain barrier (BBB) in rats. METHODS:Microdialysis probes, calibrated using retrodialysis by drug, were placed into the striatum and jugular vein of seven Sprague-Dawley rats. Morphine was...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1023250900462
更新日期：2003-04-01 00:00:00
abstract：:The effect of the penetration enhancers Azone, oleic acid, 1-dodecanol, dodecyl N,N-dimethylaminoacetate (DDAA), and dodecyl N,N-dimethylaminoisopropionate (DDAIP) on epithelial membrane lipids was examined using human buccal cell membranes as a model for epithelial lipid bilayer. Buccal epithelial cells (BEC) were la...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018919811227
更新日期：1994-02-01 00:00:00
abstract：PURPOSE:To investigate the suitability of three antimicrobial peptides (AMPs) as cell-penetrating antimicrobial peptides. METHODS:Cellular uptake of three AMPs (PK-12-KKP, SA-3 and TPk) and a cell-penetrating peptide (penetratin), all 5(6)-carboxytetramethylrhodamine-labeled, were tested in HeLa WT cells and analyzed ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-014-1550-9
更新日期：2015-05-01 00:00:00
abstract：PURPOSE:To develop resource-sparing in silico approaches that aim to reduce experimental effort and material required by developability assessments (DA) of monoclonal antibody (mAb) drug candidates. METHODS:A battery of standardized biophysical experiments was performed on high concentration formulations of 16 drug pr...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-018-2466-6
更新日期：2018-08-20 00:00:00
abstract：:The effects of tertiary amine-containing basic drugs on the enzymes located in the mitochondria and the effect of monoamine oxidase inhibitors (MAOIs) on drug accumulation in lung mitochondria have been studied. Various basic drugs inhibited MAO activity but not other mitochondrial marker enzymes. The potency of MAO i...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015964623098
更新日期：1989-10-01 00:00:00
abstract：PURPOSE:Fusogenic liposomes (FLs) are unique delivery vehicles capable of introducing their contents directly into the cytoplasm with the aid of envelope glycoproteins of Sendai virus (SeV). The objective of this study was to evaluate the potential of FL to improve the mucosal absorption of insulin from rat intestinal ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-005-9175-7
更新日期：2006-02-01 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:Previously, a respirable powder (RP) formulation of pirfenidone (PFD) was developed for reducing phototoxic risk; however, PFD-RP demonstrated unacceptable in vitro inhalation performance. The present study aimed to develop a new RP system of PFD with favorable inhalation properties by spray-drying method. MET...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-016-1887-3
更新日期：2016-06-01 00:00:00
abstract：PURPOSE:The in-situ particle size of delavirdine mesylate in dry mix and tablets was determined. METHODS:Optical microscopy and fluorescence microscopy combined with image analysis were used for qualitative and quantitative measurements. RESULTS:Using optical microscopy, it was demonstrated qualitatively that fragmen...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018875130152
更新日期：1999-04-01 00:00:00
abstract：PURPOSE:In this study, we aimed to illustrate the utility of fractional radiofrequency (RF) that generated microchannels in the skin, allowing delivery of peptide and siRNA via the skin. The mechanisms involved in the correlation between macromolecule permeation and skin structure were also elucidated. METHODS:The mor...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-014-1568-z
更新日期：2015-05-01 00:00:00
abstract：PURPOSE:The purpose of this work was to study the influence of cell differentiation on the mRNA expression of transporters and channels in Caco-2 cells and to assess Caco-2 cells as a model for carrier-mediated drug transport in the intestines. METHOD:Gene mRNA expression was measured using a custom-designed microarra...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1022282221530
更新日期：2003-01-01 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 determine of the pharmacokinetic profile of methotrexate (MTX) in blood and extracellular fluid (ECF) of VX2 tumor and muscle in rabbits. METHODS:Microdialysis probes were inserted into VX2 tumor and in muscle tissue. Following intravenous administration of MTX (30 mg/kg), serial collection of arterial bloo...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1011973409022
更新日期：1998-01-01 00:00:00
abstract：:The influence of varying protein and fat content in milk of New Zealand White rabbits on the milk-to-plasma drug concentration (M/P) ratio of diazepam was studied. At various time points after littering, a bolus dose (1.5 mg/kg) followed by a 26-hr infusion (1.8 mg/h) of diazepam was administered to freely moving rabb...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015809418284
更新日期：1992-10-01 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:Nine common excipients were examined to determine their ability to cause disproportionation of the HCl salt of a a weakly basic compound. The goal was to determine which excipients were problematic and correlate the results to known properties such as surface pH, slurry pH, or molecular structure. Such a correl...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-013-1002-y
更新日期：2013-06-01 00:00:00
abstract：:Short-lived gamma emitting radioisotopes can be incorporated into polylactide/glycolide polymeric microspheres with various specific activities for possible use in understanding the in-vivo deposition, distribution and clearance of microparticulate drug carrier systems. The incorporated radiolabel is stable with negli...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1016237216352
更新日期：1995-12-01 00:00:00
abstract：PURPOSE:A double-mutant E224A/E262A full-length botulinum neurotoxin (BoNT) Type A with structural similarity to native BoNT/A but lacking the endopeptidase activity provides an ideal surrogate for testing pharmacokinetics and immunochemical characteristics of BoNT. METHODS:We determined lethality (LD50) of deactivate...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-015-1816-x
更新日期：2016-03-01 00:00:00
abstract：PURPOSE:A mechanism-based PK-PD model was developed to predict the time course of dopamine D(2) receptor occupancy (D(2)RO) in rat striatum following administration of olanzapine, an atypical antipsychotic drug. METHODS:A population approach was utilized to quantify both the pharmacokinetics and pharmacodynamics of ol...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-011-0477-7
更新日期：2011-10-01 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
