Novel core-shell dual-mesoporous silica nanoparticles (DMSN) were successfully prepared as a carrier in order to improve the dissolution of fenofibrate and obtain an oral highly bioavailable controlled-release drug delivery system using the osmotic pump technology. Fenofibrate was loaded into DMSN by an adsorption method. The solid state properties of fenofibrate in DMSN, before and after drug loading, were characterized by scanning electron microscopy (SEM), transmission electron microscopy (TEM), nitrogen adsorption/desorption analysis (BET), thermogravimetric analysis (TGA), Fourier transform infrared spectroscopy (FTIR), X-ray powder diffraction (XRD) and differential scanning calorimetry (DSC). In vitro release tests showed that DMSN increased the dissolution rate of fenofibrate and produced zero-order release in push–pull osmotic pump tablets (OPT). The relative bioavailability of OPT was 186.9% in comparison with the commercial reference product. In summary, osmotic pump technology in combination with solid dispersion technology involving nanometer materials is a promising way for achieving the oral delivery of poorly water-soluble drugs. 相似文献
Applications of hydrophobic drug‐based nanocarriers (NCs) remain largely limited because of their low loading capacity. Here, development of a multifunctional hybrid NC made of a magnetic Fe3O4 core and a mesoporous silica shell embedded with carbon dots (CDs) and paclitaxel (PTX), and covered by another layer of silica is reported. The NC is prepared via a one‐pot process under mild condition. The PTX loading method introduced in this study simplifies drug loading process and demonstrates a high loading capacity due to mesoporous silica dual‐shell structure, supramolecular π‐stacking between conjugated rings of PTX molecules, and aromatic rings of the CDs in the hybrid NC. The CDs serve as both confocal and two‐photon fluorescence imaging probes, while the Fe3O4 core serves as a magnetic resonance imaging contrast agent. Significantly, NC releases PTX in response to near infrared irradiation as a result of local heating of the embedded CDs and the heating of CDs also provides an additional therapeutic effect by thermally killing cancer cells in tumor in addition to the chemotherapeutic effect of released PTX. Both in vitro and in vivo results show that NC demonstrates high therapeutic efficacy through a synergistic effect from the combined chemo‐photothermal treatments. 相似文献
Phospholipid bilayers represent a complex, anisotropic environment fundamentally different from bulk oil or octanol, for instance. Even “simple” drug association to phospholipid bilayers can only be fully understood if the slab‐of‐hydrocarbon approach is abandoned and the complex, anisotropic properties of lipid bilayers reflecting the chemical structures and organization of the constituent phospholipids are considered. The interactions of drugs with phospholipids are important in various processes, such as drug absorption, tissue distribution, and subcellular distribution. In addition, drug–lipid interactions may lead to changes in lipid‐dependent protein activities, and further, to functional and morphological changes in cells, a prominent example being the phospholipidosis (PLD) induced by cationic amphiphilic drugs. Herein we briefly review drug–lipid interactions in general and the significance of these interactions in PLD in particular. We also focus on a potential causal connection between drug‐induced PLD and steatohepatitis, which is induced by some cationic amphiphilic drugs.相似文献
Pilot plant experiments applying solar titanium dioxide photocatalysis and solar photo-Fenton treatment at different pH and iron concentrations with an initial diclofenac concentration of 50 mg L−1 are described.
In preliminary experiments absence of hydrolysis and slow photolysis under solar irradiation of diclofenac solutions were observed. Solar photo-Fenton treatment with freshly precipitated iron at pH around 7 showed first order kinetics, the reaction taking place on the surface of the iron precipitate. Simultaneous oxidation, precipitation and re-dissolution processes of diclofenac governed photo-Fenton decomposition kinetics at pH 2.8. The use of different iron concentrations (0.03–0.75 mM) showed no influence on the reaction rate in a neutral medium due to reactor geometry. Similar behaviour (no influence of iron concentration) was observed at pH 2.8, due to precipitation problems. A pH of around 4, close to the pKa of diclofenac, showed promising results, partly overcoming both iron and diclofenac precipitation. Solar titanium dioxide photocatalysis with Degussa P-25 followed first order kinetics and no precipitation or adsorption occurred.
Decomposition of diclofenac took around 100 min under all photo-Fenton treatment conditions employed. Decomposition by titanium dioxide photocatalysis took about 200 min. In photo-Fenton treatment, hydrogen peroxide consumption to diclofenac decomposition was about 80–110 mM at pH 2.8 and 40 mM in the other two treatments (neutral pH and pH = 4). 相似文献
W. J. Lynch and M. E. Carroll's (see record 2001-06653-001) review argues aversive effects and for satiation and direct effects as the mechanisms responsible for the descending limb of the dose-response function. Analysis is provided that suggests they may prematurely dispose of the aversive-effects account. Further analysis of the evidence for satiation and direct effects supports the authors' contention that neither can be exclusively supported. A brief behavioral–economic analysis of drug-intake regulation and the descending limb of the dose-response function is presented. (PsycINFO Database Record (c) 2010 APA, all rights reserved) 相似文献