Post-modulation of layer-by-layer assemblies coordinated by a catalytic dose of fullerene derivatives without external fields.

Molecular assembly has attracted wide attention in chemistry, condensed physics, molecular electronics, and materials sciences. However, it remains a great challenge to perform post-modulation on the assembled structures without the aid of externally applied fields. Herein, we demonstrate a combined full-weak-bonded interaction and fullerene-derivative strategy and achieve the post-modulation of layer-by-layer assembly with a precision of 5.

Development of flurbiprofen-loaded nanoparticles with a narrow size distribution using sucrose.

Objective: A novel flurbiprofen-loaded nanoemulsion which gave uniform emulsion droplets with a narrow size distribution was previously reported to be prepared using membrane emulsification method. The purpose of this study is to develop a novel flurbiprofen-loaded nanoparticle with a narrow size distribution and improved bioavailability.

Method: The nanoparticle was prepared by solidifying nanoemulsion using sucrose as a carrier via spray drying method.

Development and optimization of self-nanoemulsifying drug delivery system with enhanced bioavailability by Box-Behnken design and desirability function.

The aim of our study was to characterize and optimize a self-nanoemulsifying drug delivery system (SNEDDS) formulation by a three-factor, three-level Box-Behnken design (BBD) combined with a desirability function. The independent factors were the amounts of Capryol PGMC (X(1)), Tween 20 (X(2)), and Transcutol HP (X(3)). The dependent variables were droplet size (Y(1)), equilibrium solubility (Y(2)), and cumulative percentage of drug released in 15 min (Y(3)) from the SNEDDS formulation.

Lipid emulsion as a drug delivery system for breviscapine: formulation development and optimization.

In this study, we developed an optimized formulation of a breviscapine lipid emulsion (BLE) and evaluated the physicochemical properties and in vivo pharmacokinetics of BLE in rats. For the preparation of the lipid emulsion, soybean oil and oleic acid were used as the oil phase, lecithin and poloxamer 188 as surfactants and glycerol as co-surfactant. An optimized formulation consisting of soybean oil (10.

Effect of dose and dosage interval on the oral bioavailability of docetaxel in combination with a curcumin self-emulsifying drug delivery system (SEDDS).

The present study investigated the effects of a curcumin self-emulsifying drug delivery systems (SEDDS) on the pharmacokinetics of orally administered docetaxel in rats. A single dose of docetaxel was orally administered (30 mg/kg) alone or after oral curcumin SEDDS (25, 50, 100 and 150 mg/kg) administration with time intervals of 0, 15 and 30 min, respectively. After oral administration, the C (max) and the area under the plasma concentration-time curve (AUC) of docetaxel were significantly increased (0 min, p < 0.

Novel valsartan-loaded solid dispersion with enhanced bioavailability and no crystalline changes.

With the aim of developing a novel valsartan-loaded solid dispersion with enhanced bioavailability and no crystalline changes, various valsartan-loaded solid dispersions were prepared with water, hydroxypropyl methylcellulose (HPMC) and sodium lauryl sulphate (SLS). Effects of the weight ratios of SLS/HPMC and carrier/drug on both the aqueous solubility of valsartan and the drug-release profiles of solid dispersions were investigated. The physicochemical properties of solid dispersions were characterized using scanning electron microscope (SEM), differential scanning calorimetry (DSC) and X-ray diffraction (XRD).

Evaluation of physicochemical properties, skin permeation and accumulation profiles of salicylic acid amide prodrugs as sunscreen agent.

Various amide prodrugs of salicylic acid were synthesised, and their physicochemical properties including lipophilicity, chemical stability and enzymatic hydrolysis were investigated. In vivo skin permeation and accumulation profiles were also evaluated using a combination of common permeation enhancing techniques such as the use of a supersaturated solution of permeants in an enhancer vehicle, a lipophilic receptor solution, removal of the stratum corneum and delipidisation of skin. Their capacity factor values were proportional to the degree of carbon-carbon saturation in the side chain.

Enhanced oral bioavailability of curcumin via a solid lipid-based self-emulsifying drug delivery system using a spray-drying technique.

In this study, a novel liquid self-emulsifying drug delivery system (SEDDS) containing curcumin was formulated and further developed into a solid form by a spray drying method using Aerosil 200 as the solid carrier. The optimum liquid SEDDS consisted of Lauroglycol Fcc, Labrasol and Transcutol HP as the oil phase, the surfactant and the co-surfactant at a weight ratio of 15.0 : 70.

Preparation and evaluation of Cremophor-free paclitaxel solid dispersion by a supercritical antisolvent process.

Objectives: To avoid the major adverse effects induced by Cremophor EL formulated in the commercial paclitaxel products of Taxol.

Methods: An injectable paclitaxel solid dispersion free of Cremophor was prepared by a supercritical antisolvent process and then was fully characterized and investigated with regard to its short-term and long-term stability. Pharmacokinetics in rats was also evaluated compared with the commercial product.

Development of thermo-sensitive injectable hydrogel with sustained release of doxorubicin: rheological characterization and in vivo evaluation in rats.

To develop a thermo-sensitive injectable hydrogel that is easy to administer, gels quickly in the body, and allows sustained release of the drug, various poloxamer-based hydrogels containing doxorubicin were prepared with poloxamer and hydrochloric acid under light protection using the cold method. Their rheological characterization, dissolution, and pharmacokinetics after intramuscular administration to rats were evaluated. Hydrochloric acid decreased the viscosity and retarded the gelation time of the injectable gel.

The physicochemical properties, in vitro metabolism and pharmacokinetics of a novel ester prodrug of EXP3174.

EXP3174 is the major active metabolite of losartan, a drug currently widely used for the treatment of cardiovascular diseases. This study was designed to evaluate the physicochemical properties of EXP3174-pivoxil (a novel synthesized prodrug of EXP3174) and characterize its metabolism, regional intestinal absorption and pharmacokinetics by in vitro and in vivo studies. An in vitro metabolism study was conducted in liver and intestinal S9 fractions from different species including rat, dog and human.

Enhanced oral bioavailability of docetaxel in rats by four consecutive days of pre-treatment with curcumin.

As with many other anti-cancer agents, docetaxel is a substrate for ATP-binding cassette transporters such as P-glycoprotein and its metabolism is mainly catalysed by CYP3A. In order to improve the oral bioavailability of docetaxel, a component of turmeric, curcumin, which can down-regulate the intestinal P-glycoprotein and CYP3A protein levels, was used for the pre-treatment of rats before the oral administration of docetaxel. Curcumin (100 mg/kg) did not significantly modify the pharmacokinetics of docetaxel when given orally 30 min before the administration of docetaxel.

Preparation and evaluation of taste-masked donepezil hydrochloride orally disintegrating tablets.

The purpose of this research was to prepare and evaluate a non-bitter donepezil hydrochloride (DH) orally disintegrating tablet (ODT) for enhanced patient compliance. Taste masking was done by preparing microspheres with different ratios of drug and Eudragit EPO using spray drying method. The entrapment of the drug into microspheres was confirmed by scanning electron microscope (SEM) and X-ray powder diffraction.

Development of valsartan-loaded gelatin microcapsule without crystal change using hydroxypropylmethylcellulose as a stabilizer.

To develop a valsartan-loaded gelatin microcapsule using hydroxypropylmethylcellulose (HPMC) as a stabilizer, which could improve the physical stability and bioavailability of valsartan, the gelatin microcapsules were prepared with various ratios of gelatin and HPMC using a spray-drying technique. Their solubility, dissolution, thermal characteristics, crystallinity, and physical stability were investigated. The bioavailability of drug in valsartan-loaded microcapsule was then evaluated compared to drug powder and commercial product in rats.

Enhanced oral bioavailability of flurbiprofen by combined use of micelle solution and inclusion compound.

The main purpose of this study was to evaluate the effect of a mixed drug solution containing a surfactant and beta-cyclodextrin (beta-CD) on the solubility and bioavailability of a poorly water soluble drug, flurbiprofen. Solubility, dissolution and in vivo pharmacokinetics of flurbiprofen in the presence of surfactant, beta-CD or mixture of surfactant and beta-CD were investigated. Among the surfactants tested, Tween 80 produced the highest improvement in the aqueous solubility of flurbiprofen.