Cyanine derivative as a suitable marker for thermosensitive in situ gelling delivery systems: In vitro and in vivo validation of a sustained buccal drug delivery.

Buccal administration route is a promising way for a large number of drugs exhibiting a low oral bioavailability. The present work describes the formulation and evaluation of a mucoadhesive and thermosensitive in situ gelling delivery system based on poloxamer 407, poloxamer 188 and xanthan gum for buccal drug delivery. First, the mucoadhesion properties were evaluated using a tensile test.

Poloxamer bioadhesive hydrogel for buccal drug delivery: Cytotoxicity and trans-epithelial permeability evaluations using TR146 human buccal epithelial cell line.

A salbutamol sulfate (SS)-Poloxamer bioadhesive hydrogel specially developed for buccal administration was investigated by studying interactions with TR146 human buccal epithelium cells (i.e. cellular toxicity (i) and trans-epithelial SS diffusion (ii)).

Influence of additives on a thermosensitive hydrogel for buccal delivery of salbutamol: relation between micellization, gelation, mechanic and release properties.

Thermosensitive hydrogels developed for buccal delivery of salbutamol were prepared using poloxamer analogs (Kolliphor(®) P407/P188), xanthan gum (Satiaxane(®) UCX930) and NaCl. P188 increased gelation temperature (Tsol-gel) by 2.5-5°C, micellization temperature (<1°C) and gelation time by >3s.

Altered HepG2 cell models using etomoxir versus tert-butylhydroperoxide.

Energetic failure which occurs in both ischemia/reperfusion and acute drug-induced hepatotoxicity is frequently associated with oxidative stress. This study displays the setting of a new cell culture model for hepatic energetic failure, i.e.

Freeze-drying of ATP entrapped in cationic, low lipid liposomes.

Concerning the instability of ATP liposomes formulated to easily diffuse through the liver (size approximately 100 nm), this work targets the key parameters that influence the freeze-drying of a preparation that combines cholesterol, DOTAP and phosphatidylcholine (either natural soybean or egg (SPC or EPC) or hydrogenated (HSPC)). After freeze-drying blank liposomes, size increased significantly when initial lipid concentration was lowered from 20 to 5mM (p=0.0018).

Formulation and evaluation of ATP-containing liposomes including lactosylated ASGPr ligand.

An original ligand (Lac-10-Chol) designed to interact with asialoglycoprotein receptors to potentially target hepatocyte was synthesised by grafting a lactose head to a cholesteryl structure, which was then included in liposomes. Preliminary formulation tests led to the selection of conventional formulations based on soybean phosphatidylcholine/cholesterol/DOTAP (+/- DOPE) (+/- Lac-10-Chol) that present reproducible absolute entrapment value (1.45 +/- 0.

L-cysteine encapsulation in liposomes: effect of phospholipids nature on entrapment efficiency and stability.

Liposomal entrapment of L-cysteine (L-CySH) could be a solution to enhance its oxidative stability and its intracellular bioavailability for glutathione (GSH) synthesis. This study addresses the influence of different factors (i.e.

A review of poloxamer 407 pharmaceutical and pharmacological characteristics.

Poloxamer 407 copolymer (ethylene oxide and propylene oxide blocks) shows thermoreversible properties, which is of the utmost interest in optimising drug formulation (fluid state at room temperature facilitating administration and gel state above sol-gel transition temperature at body temperature promoting prolonged release of pharmacological agents). Pharmaceutical evaluation consists in determining the rheological behaviour (flow curve or oscillatory studies), sol-gel transition temperature, in vitro drug release using either synthetic or physiological membrane and (bio)adhesion characteristics. Poloxamer 407 formulations led to enhanced solubilisation of poorly water-soluble drugs and prolonged release profile for many galenic applications (e.

A double-blind sham controlled study of right prefrontal repetitive transcranial magnetic stimulation (rTMS): therapeutic and cognitive effect in medication free unipolar depression during 4 weeks.

Background: Transcranial magnetic stimulation (TMS) has become a therapeutic tool in psychiatric diseases.

Methodology: The objective was to evaluate the efficacy of TMS in unipolar depression: the percentage of responders (>50% HDRS reduction) and remission (HDRS score < or =8, after four weeks of active TMS treatment in depressed patients free of any antidepressive agent versus placebo-TMS.

Results: 27 patients were randomized in two groups: rTMS (N=11) versus sham TMS (N=16).

Liver function tests during treatment with antipsychotic drugs: a case series of 23 patients.

Atypical antipsychotics represent a new class of medication for the treatment of schizophrenia and their use is associated with a reduction of neurological side effects. This article reports the result of the systematic clinical and biological supervision of hepatic enzymes on 23 schizophrenic inpatients treated by atypical antipsychotic during 2 weeks at Days 1 (D1), 7 (D7), and 14 (D14) in a naturalistic study during 6 months. The drug administrated was limited to four medications--risperidone, amisulpride, olanzapine, and clozapine--but other psychotropic agents were prescribed.