Pharmaceutical Research
1573-904X
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Các bài báo tiêu biểu
The Stability of Insulin in Crystalline and Amorphous Solids: Observation of Greater Stability for the Amorphous Form
Tập 14 Số 10 - Trang 1379-1387 - 1997
Purpose. Generalizations based upon behavior of small molecules have established
that a crystalline solid is generally much more stable toward chemical
degradation than is the amorphous solid. This study examines the validity of
this generalization for proteins using biosynthetic human insulin as the model
protein. Methods. Amorphous insulin was prepared by freeze drying the supernate
from a suspe...
Development of a Remote Electrode System for Monitoring the Water Content of Materials Inside a Glass Vial
Tập 19 Số 3 - Trang 337-344 - 2002
Purpose: This article explores the use of a remote electrode dielectric
measurement system to monitor the water content of hydrated ovalbumin inside a
glass vial. Methods: The intrinsic dielectric properties of hydrated ovalbumin
were characterized first using conventional parallel plate electrodes. The
second stage was to simulate a remote electrode measurement by placing
nonconductive, nondisper...
A Solid-State NMR Study of Protein Hydration and Stability
Tập 15 Số 12 - Trang 1816-1821 - 1998
Purpose. The mobility of protein in powders at different hydration levels was
studied in relation to aggregation and activity. Methods. Magic angle spinning
13C, 15N, 1H, 2H, and 17O NMR techniques were used to determine changes in the
mobility of surface residues in proteins as a function of hydration and related
to changes in activity. NMR relaxation measurements of high frequency (ω0, T1)
and l...
Efficiency of Cytoplasmic Delivery by pH-Sensitive Liposomes to Cells in Culture
Tập 7 Số 8 - Trang 824-834 - 1990
The intracellular processing of pH-sensitive liposomes composed of
cholesterylhemisuccinate (CHEMS) and dioleoylphosphatidylethanolamine (DOPE) by
eukaryotic cell lines has been compared to non-pH-sensitive liposomes made of
CHEMS and dioleoylphosphatidylcholine (DOPC). The pH-sensitive liposomes can
deliver encapsulated fluorescent molecules [calcein, fluoresceinated dextran,
fluoresceinated poly...
Stability of Protein Formulations: Investigation of Surfactant Effects by a Novel EPR Spectroscopic Technique
Tập 12 Số 1 - Trang 2-11 - 1995
Surfactants are known to stabilize proteins and are often employed as additives
in protein formulations. We have developed a method to study the interaction of
these formulation additives with proteins by using the partitioning behavior of
a spin label. In protein-free formulations, 16-doxyl stearic acid partitions
into micelles above the critical micelle concentration (CMC) of the surfactant
and ...
Effect of Some Penetration Enhancers on Epithelial Membrane Lipid Domains: Evidence from Fluorescence Spectroscopy Studies
Tập 11 Số 2 - Trang 288-294 - 1994
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 labeled with l,6-diphenyl-l,3,5-hexatriene (DPH),
l-(4-(trimethylammonio)phenyl)-6-...
Inhibition of the Friend Retrovirus by Antisense Oligonucleotides Encapsulated in Liposomes: Mechanism of Action
Tập 10 Số 10 - Trang 1427-1433 - 1993
Proliferation of the Friend retrovirus was specifically inhibited by the env
mRNA complementary oligonucleotide encapsulated in pH-sensitive liposomes. This
observation was made using the focus immunoassay (FIA) and the reverse
transcriptase test. The key finding of the present study was the dramatic impact
on liposome penetration. For chronic or de novo infection, the point at which
the penetrati...
Supersaturation: Enhancement of Skin Penetration and Permeation of a Lipophilic Drug
Tập 18 Số 7 - Trang 1006-1011 - 2001
Purpose. To increase the dermal delivery of a lipophilic model compound (LAP),
and to deduce the underlying mechanism of enhanced absorption. Methods.
Penetration of LAP from mixtures of up to four degrees of saturation into the
stratum corneum was evaluated using a tape-stripping method; epidermal
permeation of the drug was measured in Franz diffusion cells. The relative
diffusion and stratum cor...
Uptake of FITC-Chitosan Nanoparticles by A549 Cells
Tập 19 Số 10 - Trang 1488-1494 - 2002
Purpose. The objective of this study was to evaluate the extent and mechanism of
uptake of fluorescent chitosan nanoparticles by the A549 cells, a human cell
line derived from the respiratory epithelium. Methods. Covalent conjugation with
fluorescein-5-isothiocyanate yielded stably labeled chitosan molecules, which
were successfully formulated into nanoparticles by ionotropic gelation. Uptake
of f...
β-Adrenergic Receptor Polymorphisms: Cardiovascular Disease Associations and Pharmacogenetics
Tập 19 Số 12 - Trang 1779-1787 - 2002
The β-adrenergic receptors (βAR) play important roles in cardiovascular function
and disease, and both agonists and antagonists are widely used in various
settings for treatment of cardiovascular disease. Both the β1AR and β2AR genes
have several polymorphisms that are common in the population and result in
encoding of different amino acids. More importantly, in vitro functional studies
suggest th...