Journal of Pharmaceutical Sciences
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Determination of the optimal cell-penetrating peptide sequence for intestinal insulin delivery based on molecular orbital analysis with self...
We sought to determine the CPP that most effectively enhanced intestinal insulin absorption. An in situ loop absorption study using 26 penetratin analogues suggested that the chain length, hydrophobicity, and amphipathicity of the CPPs, as well as their basicity, contribute to their absorption-enhan...
Effects of submicron particles on formation of micron-sized particles during long-term storage of an interferon-beta-1a solution.
We present evidence that homogeneous submicron particles can influence the growth rate of larger particles upon long-term storage in a temperature-dependent manner. Interferon-beta-1a was thermally stressed at 50°C for 6 h and characterized using nanoparticle tracking analysis (NTA), microflow digi...
Solubility prediction of drugs in mixed solvents using partial solubility parameters
Solubility of drugs in binary and ternary solvent mixtures composed of water and pharmaceutical cosolvents at different temperatures were predicted using the Jouyban-Acree model and a combination of partial solubility parameters as interaction descriptors in the solution. The general...
PhRMA CPCDC initiative on predictive models of human pharmacokinetics, part 1: Goals, properties of the PhRMA dataset, and comparison with l...
This study is part of the Pharmaceutical Research and Manufacturers of America (PhRMA) initiative on predictive models of efficacy, safety, and compound properties. The overall goal of this part was to assess the predictability of human pharmacokinetics (PK) from preclinical data and...
PLGA microdevices for retinoids sustained release produced by supercritical emulsion extraction: Continuous versus batch operation layouts
Retinyl acetate (RA) was selected as a model compound to be entrapped in poly(lactic-co-glycolic)acid (PLGA) microspheres using supercritical emulsion extraction (SEE). Several oil-in-water emulsions prepared using acetone and aqueous glycerol (80% glycerol, 20% water) were processed...
Prolonged circulation half-life of interferon γ activity by gene delivery of interferon γ-serum albumin fusion protein in mice.
We tried to increase the circulation half-life of IFNγ after its gene delivery by designing a novel fusion protein of IFNγ with mouse serum albumin (MSA). Western blot analysis confirmed that IFNγ-MSA was expressed as a fusion protein, but hardly formed dimer as IFNγ did. The biological activity...
Usefulness of a nanoparticle formulation to investigate some hemodynamic parameters of a poorly soluble compound.
Drug solubility is an important issue when progressing investigational compounds into clinical candidates. The present paper describes the development and characterization of a nanosuspension that was formulated to overcome problems with poor water solubility and possible adverse events caused by cos...
Lengthening of cardiac repolarization in isolated guinea pigs hearts by sequential or concomitant administration of two IKr blockers.
Block of I(Kr) is of major concern in drug safety. The objective of this study was to assess prolongation of cardiac repolarization during the combined use of two I(Kr) blockers when administered concomitantly or sequentially. (1) When isolated hearts from male guinea pigs were perfused concomitantly...
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Polyamidoamine dendrimers can improve the pulmonary absorption of insulin and calcitonin in rats.
The absorption-enhancing effects of polyamidoamine (PAMAM) dendrimers with various generations (G0-G3) and concentrations [0.1%-1.0% (w/v)] on the pulmonary absorption of peptide and protein drugs were studied in rats. Insulin and calcitonin were chosen as models of peptide and prote...