Pharmaceutical Research
1573-904X
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In Vivo and in Vitro Assessment of Baseline Blood-Brain Barrier Parameters in the Presence of Novel Nanoparticles
Tập 20 Số 5 - Trang 705-713 - 2003
Purpose. Nanoparticles have advantage as CNS drug delivery vehicles given they
disguise drug permeation limiting characteristics. Conflicting toxicological
data, however, is published with regard to blood-brain barrier integrity and
gross mortality. Methods. To address this issue two novel nanoparticle types:
“emulsifying wax/Brij 78”and Brij 72/Tween 80 nanoparticles were evaluated in
vivo for ef...
Monitoring Microviscosity and Microacidity of the Albumin Microenvironment Inside Degrading Microparticles from Poly(lactide-co-glycolide) (PLG) or ABA-triblock Polymers Containing Hydrophobic Poly(lactide-co-glycolide) A Blocks and Hydrophilic Poly(ethyleneoxide) B Blocks
Tập 15 Số 5 - Trang 787-793 - 1998
Purpose. The purpose of this study was to monitor the microenvironment of an
encapsulated model protein during the release from biodegradable microparticles
(MP) made from three different polymers, namely poly(lactide-co-glycolide) (PLG)
and ABA-triblock polymers containing hydrophobic poly(lactide-co-glycolide) A
blocks and hydrophilic poly(ethyleneoxide) B blocks with an A:B ratio of 90:10
(ABA1...
Passive and Carrier-Mediated Intestinal Absorption Components of Two Angiotensin Converting Enzyme (ACE) Inhibitor Prodrugs in Rats: Enalapril and Fosinopril
Tập 6 Số 12 - Trang 1043-1047 - 1989
The intestinal absorption mechanism of two ACE inhibitor prodrugs, enalapril and
fosinopril, was investigated in rats using a single-pass perfusion method. A
modified boundary layer solution was applied to determine the apparent
intestinal wall permeability. The prodrug enalapril is well absorbed from rat
jejunum, whereas the parent drug, enalaprilat, is poorly absorbed. The
permeability of enalap...
Use of Solid Corrugated Particles to Enhance Powder Aerosol Performance
Tập 18 Số 11 - Trang 1570-1577 - 2001
Purpose. To study the dispersion performance of non-porous corrugated particles,
with a focus on the effect of particle surface morphology on aerosolization of
bovine serum albumin (BSA) powders. Methods. The solid-state characteristics of
the spray-dried BSA powders, one consisting of smooth spherical particles and
another corrugated particles, were characterized by laser diffraction, X-ray
powde...
P-Glycoprotein Inhibition Leads to Enhanced Disruptive Effects by Anti-Microtubule Cytostatics at the In Vitro Blood-Brain Barrier
Tập 18 Số 5 - Trang 587-592 - 2001
Purpose. To investigate whether P–glycoprotein (Pgp) protects the in vitro BBB
against the cytotoxic effects of anti–tumour drugs. Methods. In an in vitro BBB
coculture model the influence of the anti–microtubule drugs vinblastine,
colchicine, paclitaxel and the non–antimicrotubule drugs doxorubicin,
fluorouracil and etoposide in the absence or presence of Pgp modulators on the
trans–endothelial e...
Intestinal Transport of β-Lactam Antibiotics: Analysis of the Affinity at the H+/Peptide Symporter (PEPT1), the Uptake into Caco-2 Cell Monolayers and the Transepithelial Flux
Tập 16 Số 1 - Trang 55-61 - 1999
Purpose. This study on the intestinal transport of β-lactam antibiotics was
undertaken to investigate the correlation between cellular transport parameters
and the bioavailability. Methods. Transport of 23 β-lactam antibiotics was
characterized by measuring their ability to inhibit the uptake of
glycylsarcosine into Caco-2 cells, their uptake into the cells and their total
flux across the cell mon...
Physical Entrapment of Adriamycin in AB Block Copolymer Micelles
Tập 12 Số 2 - Trang 192-195 - 1995
The entrapment of Adriamycin (ADR) in micelles composed of AB block copolymers
(poly(ethylene oxide-co-β-benzyl L-aspartate) (PEO-PBLA)) was investigated. The
loading process involved transfer of ADR and PEO-PBLA into an aqueous milieu
from dimethyl-formamide (DMF) through a dialysis procedure. Evidence for the
physical entrapment of ADR in the polymeric micelles was derived from
fluorescence spec...
Protein–Solvent Interactions in Pharmaceutical Formulations
Tập 8 Số 3 - Trang 285-291 - 1991
The stability of proteins is affected by a variety of solvent additives. Sugars,
certain amino acids and salts, and polyhydric alcohols stabilize proteins in
solution and during freeze-thawing. Urea and guanidine hydrochloride destabilize
proteins under either condition. These effects can be explained from the
preferential interactions of the cosolvents with the proteins; i.e., the protein
stabili...
Formulation and Physical Characterization of Large Porous Particles for Inhalation
Tập 16 Số 11 - Trang 1735-1742 - 1999
Purpose. Relatively large (>5 µm) 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 endogenous to the lungs; and second, to compare the aerodynamic
size and performance of the...