Journal of Pharmaceutical Sciences
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Methyl-Beta-cyclodextrins: the role of number and types of substituents in solubilizing power.
We compared various methylated β-CDs concerning their structure characterized by nuclear magnetic resonance spectroscopy, composition analyzed by HPLC and solubilizing capability by using model compounds such as cholesterol, fatty acids, furosemide, tamoxifen, and amiodarone. All the commercially av...
Oil-in-Oil-Emulsions with Enhanced Substantivity for the Treatment of Chronic Skin Diseases.
We therefore developed oil-in-oil-emulsions that deliver the active pharmaceutical ingredient (API) to the skin over a prolonged period of time. In this study, we compare the permeation of the API from a conventional formulation to its permeation from an oil-in-oil-emulsion under infinite and finite...
Pretreatment with skin permeability enhancers: importance of duration and composition on the delivery of diclofenac sodium.
The use of chemical penetration enhancers (CPEs) is one of the most common approaches to improve the dermal and transdermal delivery of drugs. However, often, incorporation of CPEs in the formulation poses compatibility and stability challenges. Moreover, incorporation of enhancers in the formulatio...
Toward an improved understanding of the precipitation behavior of weakly basic drugs from oral lipid-based formulations.
These results suggested that in vitro conditions (dispersive versus digestive) largely influenced the solid-state properties of precipitating weak bases. Solid-state characterization of precipitated drugs under different experimental conditions should be routinely performed in formulation screening...
Overcoming Multidrug Resistance in 2D and 3D Culture Models by Controlled Drug Chitosan-Graft Poly(Caprolactone)-Based Nanoparticles.
The principal limitations of chemotherapy are dose-limiting systemic toxicity and the development of multidrug-resistant phenotypes. The aim of this study was to investigate the efficiency of a new sustained drug delivery system based on chitosan and ε-caprolactone to overcome multidrug resistance i...
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...