AimThe aim of the present study was to develop nanoproliposomes of lercanidipine, in order to overcome its poor biopharmaceutical properties and to improve its therapeutic efficacy in treating hypertension.

Lercanidipine is a vasoselective dihydropyridine calcium antagonist, mainly used for the treatment of hypertension and angina pectoris. However, it suffers from food dependent absorption, poor solubility, low permeability and considerable first pass metabolism, resulting in highly variable and l...

An improved and reliable ultra-performance liquid chromatography/tandem mass spectrometry (UPLC–MS/MS) method has been developed and validated for the determination of lercanidipine in human plasma. Plasma samples with lercanidipine-d3 as an internal standard (IS) were prepared by solid phase e...

Lercanidipine (LERCA) is a third generation antihypertensive drug belonging to the 1,4-dihydropyridine’s family, which has been reported to induce photoallergic and/or phototoxic effects in patients with long term treatment. The electronic nature of substituents on the 4-aryl moiety bonded to t...

Poorly water-soluble drugs pose the problem of low availability due to their limited solubility in the varying pH of the gastrointestinal tract (GIT). The aim of the present study was to develop a pH-dependent gradient-release drug delivery system for a poorly water-soluble drug, Lercanidipine H...

The current investigation was aimed to improve the solubility of poorly soluble lercanidipine hydrochloride as self emulsifying powder (SEP). Liquid SEDDS of LCH was formulated with Capmul MCM L8 as oil, Tween (R) 80 as surfactant and PEG 400 as co surfactant after screening various vehicles. Th...

The aim of current research was to develop and characterize solid self-emulsified nanostructures (S-SEN) loaded with a BCS class II drug, Lercanidipine hydrochloride (LCH). The liquid self-emulsified nanostructures (L-SEN) were prepared using rice bran oil and glyceryl monooleate (GMO) as oil ph...

Lercanidipine hydrochloride is a calcium channel blocker used in the treatment of hypertension. It is a poor water soluble drug with absolute bioavailability of 10%. The aim of this study was to design lercanidipine hydrochloride-loaded nanostructured lipid carriers to investigate whether the bi...

A new simple, precise, accurate, and selective high performance thin-layer chromatographic (HPTLC) method has been developed for analysis of lercanidipine hydrochloride (LER) in a tablet, using chloroform:toluene:methanol:acetic acid (8:1:1:1; v/v/v/v) as mobile phase. Chromatographic separation...

During maturation and ageing in oak barrels wines improve their organoleptic properties. Ellagitannins can be released from wood to the wine and be involved in oxidation reactions and seem to influence the astringency and colour properties of the wine.Nevertheless, the ellagitannins levels are l...

A new method for the analysis of ellagitannins observed in oak-aged wine is proposed, exhibiting interesting advantages with regard to previously reported analytical methods. The necessary extraction of ellagitannins from wine was simplified to a single step of solid phase extraction (SPE) using...

Three ellagitannins from Quercus robur wood have been studied by high resolution 1H and 13C NMR. Two are the epimeric 1,2,3,5-nonahydroxytriphenoyl-4,6-hexahydroxydiphenoyl-glucoses, castalagin and vescalagin. The third is a dimeric compound, roburin A, composed of two vescalagin subunits probab...

Class III antiarrhythmic agents selectively delay the effective refractory period (ERP) and increase the transmembrance action potential duration (APD). Based on our previous studies, a set of 17 methylsulfonamido phenylethylamine analogues were investigated by 3D-QSAR techniques of CoMFA and Co...

Some aromatic O-alkyloxime ethers substituted with methylsulfonamido (7) or methylsulfonyl (8) groups on their aliphatic portions were prepared as analogues of structurally related cyclooxygenase (COX) inhibitors (6) bearing a carboxylic group typical of the classic non-steroidal anti-inflammato...

2-Hydroxy-2-(ethoxyphenylphosphinyl)acetic acid, a new type of organophosphorus compound possessing two stereogenic centers, was investigated. Racemic 2-butyryloxy-2-(ethoxyphenylphosphinyl)acetic acid was synthesized and hydrolyzed using four bacterial species as biocatalysts. In all cases the ...

A donor acceptor substituted aromatic system 5-(4-dimethylamino-phenyl)-penta-2,4-dienoic acid (DMAPPDA) has been synthesized and its spectral properties have been explored on the basis of steady state absorption and fluorescence spectroscopy. Spectral features point largely towards a possible o...

The N-unsubstituted 4-aryl-1H-1,2,3-triazoles were synthesized via the acetic acid promoted cycloaddition between β-nitrostyrenes with sodium azide under transition-metal-free conditions in a continuous flow microreactor. The continuous-flow microreactor provided a safe environment for the dang...

The emergence and global spread of metallo-β-lactamase (MBL) mediated resistance to almost all β-lactam antibacterials poses a serious threat to public health. Since no clinically useful MBL inhibitors have been reported, there is an urgent need to develop new potent broad-spectrum MBL inhibit...

A series of push-pull aryl-bithiophene based systems 2–3 were designed and synthesized in order to understand how structural modifications influence the electronic, linear and nonlinear optical properties. The push-pull conjugated chromophores 2–3 bear a bithiophene spacer conjugated with a ph...

A method for the synthesis of long chain fatty acids substituted at the ω and ω-1 positions has been developed. The key step is the isomerization of the triple bond of an alkyn-1-ol from an internal position in the chain to the free terminus with a new, convenient reagent, sodium aminopropylam...