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PubMed Journal Database | European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences RSS

09:08 EDT 27th May 2019 | BioPortfolio

The US National Library of Medicine and National Institutes of Health manage PubMed.gov which comprises of more than 29 million records, papers, reports for biomedical literature, including MEDLINE, life science and medical journals, articles, reviews, reports and  books.

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Showing PubMed Articles 1–25 of 629 from European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences

The influence of core tablets rheology on the mechanical properties of press-coated tablets.

Press-coating (also called compression coating or dry coating) consists of a second compression of an outer layer of material over a preformed tablet core. Despite being old, this technology has returned to popularity due to its widespread use in preparation of chronotherapeutic dosage forms. The literature available on press-coated tablets has mainly investigated drug release kinetics, while there is a lack of information about their mechanical properties. Here we study, for the first time, the effect of m...

Digital light processing (DLP) 3D-printing technology and photoreactive polymers in fabrication of modified-release tablets.

In this study, we assessed the feasibility of using digital light processing (DLP) 3D printers (3DP) in fabrication of solid oral dosage forms. The DLP technology uses a digital micromirror device (DMD) that reflects and focuses ultraviolet (UV) light on the surfaces of photoreactive materials that polymerize in a layer-by-layer fashion. Using poly(ethylene glycol) diacrylate (PEGDA) and poly(ethylene glycol) dimethacrylate (PEGDMA) as photoreactive polymers and theophylline as a model drug, we deployed a D...

Use of prior knowledge and extrapolation in paediatric drug development: A case study with deferasirox.

The characterisation of pharmacokinetics, pharmacodynamics and dose-exposure-response relationships requires data arising from well-designed study protocols and a relatively large sample from the target patient population. Such a prerequisite is unrealistic for paediatric rare diseases, where the patient population is often vulnerable and very small. In such cases, different sources of data and knowledge need to be considered to ensure trial designs are truly informative and oncoming data can be analysed ef...

Microdosed midazolam for the determination of cytochrome P450 3A activity: Development and clinical evaluation of a buccal film.

Cytochrome P450 3A (CYP3A) isozymes metabolize about 50% of all marketed drugs. Their activity can be modulated up to 400-fold, which has great impact on individual dose requirements for CYP3A substrates. The activity of CYP3A can be monitored using the CYP3A substrate midazolam. To avoid pharmacological midazolam effects during phenotyping, a microdosing approach is preferred. However, the preparation of microdosed dosage forms remains a challenge. Fast dissolving buccal films are therefore proposed to fac...

Er:YAG fractional laser ablation for cutaneous co-delivery of pentoxifylline and d-α-tocopherol succinate: A new approach for topical treatment of radiation-induced skin fibrosis.

Radiation induced fibrosis is a common side-effect after radiotherapy. Pentoxifylline is reported to reverse radiation injuries when used in conjunction with D-α-tocopherol. However, pentoxifylline has a short half-life, limited oral bioavailability, and induces several systemic adverse effects. The objective of this study was to investigate the feasibility of using Er:YAG fractional laser ablation to enable simultaneous cutaneous delivery of pentoxifylline and D- α -tocopherol succinate from poly(lactide...

Curcumin ameliorates the targeted delivery of methotrexate intercalated montmorillonite clay to cancer cells.

Montmorillonite Clay (MMT) is aimed to develop as an orally administrable drug delivery vehicle with enhanced efficacy. Aiming to enhance the therapeutic index of methotrexate, curcumin is concomitantly used with methotrexate in the present study. Being folate antagonist in nature, methotrexate is internalized into cells by folate receptor (FR); which is over-expressed in certain human cancer cells such as cervical carcinoma cells (HeLa). Firstly, montmorillonite Clay (MMT) is organically modified (OMMT) wi...

Pharmacokinetics of the SABRE agent 4,6-d-nicotinamide and also nicotinamide in rats following oral and intravenous administration.

To prepare the way for using the isotopically labelled SABRE hyperpolarized 4,6-d-nicotinamide as an MRI agent in humans we have performed an in-vivo study to measure its pharmacokinetics in the plasma of healthy rats after intravenous and oral administration. Male Han Wistar rats were dosed with either 4,6-d-nicotinamide or the corresponding control, non-labelled nicotinamide, and plasma samples were obtained at eight time points for up to 24 h after administration. Pharmacokinetic parameters were determ...

Evaluation of miscibility and polymorphism of synthetic and natural lipids for nanostructured lipid carrier (NLC) formulations by Raman mapping and multivariate curve resolution (MCR).

Nanostructured lipid carriers (NLC) belong to youngest lipid-based nanocarrier class and they have gained increasing attention over the last ten years. NLCs are composed of a mixture of solid and liquid lipids, which solubilizes the active pharmaceutical ingredient, stabilized by a surfactant. The miscibility of the lipid excipients and structural changes (polymorphism) play an important role in the stability of the formulation and are not easily predicted in the early pharmaceutical development. Even when ...

Nanostructured clay particles supplement orlistat action in inhibiting lipid digestion: An in vitro evaluation for the treatment of obesity.

Technologies that regulate energy uptake, to curb the rising trend in obesity statistics. In this study, nanostructured clay (NSC) particles, fabricated by spray drying delaminated dispersions technologies that regulate energy uptake, to curb the rising trend in obesity statistics. In this study, nanostructured clay (NSC) particles, fabricated by spray drying delaminated dispersions of commercial clay platelets (Veegum® HS and LAPONITE® XLG), were delivered as complimentary, bioactive excipients with the ...

Monitoring microsphere coating processes using PAT tools in a bench scale fluid bed.

Among the factors that influence adherence to medication within the pediatric population, taste/irritation has been identified as a critical barrier to patient compliance. With the goal of improving compliance, microspheres (matrix systems within which the drug is dispersed) can be coated with a reverse enteric polymer that will prevent the release of the drug in the oral cavity while maintaining an immediate release once the drug product reaches the stomach, thereby achieving a taste neutral profile. In th...

Pharmacophore based approach to screen and evaluate novel Mycobacterium cell division inhibitors targeting FtsZ - A modelling and experimental study.

Tuberculosis, caused by Mycobacterium tuberculosis has been one of the primal afflictions to human, and owing to the current scenario of drug resistance, newer drugs, and alternate targets are required to mitigate the disease. FtsZ is a GTP hydrolyzing protein, conserved in prokaryotes that plays a central role in Z-ring formation during cell division cytokinesis stage. This study employs the use of pharmacophore models derived from two different datasets based on Mtb-FtsZ GTPase inhibition and whole cell a...

Treatment of metastatic lung cancer via inhalation administration of curcumin composite particles based on mesoporous silica.

Curcumin attracted attention due to its promising anti-cancer properties and safety performance. However, its poor aqueous solubility and low bioavailability have to be overcome before it goes into clinic use. Here, porous composite particles are prepared by loading curcumin into mesoporous material SBA-15, and its therapeutic effect on lung cancer via inhalation administration have also been evaluated. The inclusion of curcumin in host material SBA-15 was confirmed by the reduced surface area and pore diam...

Influence of particle size and blender size on blending performance of bi-component granular mixing: A DEM and experimental study.

The effect of particle size enlargement and blender geometry down-scaling on the blend uniformity (BU) was evaluated by Discrete Element Method (DEM) to predict the blending performance of a binary granular mixture. Three 10 kg blending experiments differentiated by the physical properties specifically particle size were performed as reference for DEM simulations. The segregation behavior observed during the diffusion blending was common for all blends, while the sample BU, i.e., standard deviation of act...

Solubility and bioavailability enhancement study of lopinavir solid dispersion matrixed with a polymeric surfactant - Soluplus.

As a biopharmaceutical classification system Class IV drug, lopinavir (LPV) shows relatively poor water solubility and permeation in vivo. In the study, we developed novel solid dispersions (SD) of LPV to improve its bioavailability and to describe their overall behaviors. By employing solvent evaporation for a preliminary formulation screening, the SDs of LPV-polymer-sorbitan monolaurate (SBM, as the wetting agent) at 1:4:0.4 (w/w) dramatically enhanced the LPV dissolution in a non-sink medium, and then ho...

Multi-targeted anti-leukemic drug design with the incorporation of silicon into Nelarabine: How silicon increases bioactivity.

Acute Lymphoblastic Leukemia (ALL) represents 30% of all childhood cancers and children younger than 5 years old have the highest risk for developing ALL. Existing ALL drugs do not respond in approximately 20% of treatment. Therefore, drug development studies against ALL must be continued with either developing existing drugs or discovering new ones. In this study, we evaluated the U.S Food and Drug Administration (FDA) approved ALL drugs according to their physicochemical and pharmaceutical properties, a...

Reactive oxygen species and near-infrared light dual-responsive indocyanine green-loaded nanohybrids for overcoming tumour multidrug resistance.

The nucleus is in charge of the metabolism and heredity of the cell, and genetic mutations are closely related with tumour multidrug resistance (MDR). Indocyanine green (ICG), the FDA-approved photosensitizer, is widely used for tumour photodynamic therapy (PDT) and photothermal therapy (PTT). Few studies have clarified the cellular distribution of ICG in MDR tumour cells. In the study, ICG distribution was detected in the whole tumour cells of MCF-7 and MCF-7/ADR, especially in the nucleus, which led us to...

Topical nanostructured lipid carriers/inorganic sunscreen combination for alleviation of all-trans retinoic acid-induced photosensitivity: Box-Behnken design optimization, in vitro and in vivo evaluation.

All-trans retinoic acid is a natural retinoid and the physiologically active metabolite of vitamin A. The aim of the present study is to develop and optimize a nanostructured lipid carrier formulation to enhance the photostability of all-trans retinoic acid and alleviate its skin photosensitivity. Box-Behnken design was used for optimizing dependent variables such as particle size, zeta potential and viscosity. The total lipid (%), liquid lipid (%) and total surfactant (%) were selected as independent varia...

Quantitative analysis for lipophilic drug transport through a model lipid membrane with membrane retention.

Drug absorption after oral administration mostly occurs in the intestine, and is controlled mainly by the aqueous solubility and the intestinal permeability of the drug. In modern drug discovery, the proportion of lipophilic drug candidates with poor water solubility has increased, and these lipophilic drugs are known to undergo membrane retention during transport across the cell membrane, depending on the hydrophobic interaction between the drug and lipid molecules. Hence, a precise and effective permeabil...

Use of inspiratory profiles from patients with chronic obstructive pulmonary disease (COPD) to investigate drug delivery uniformity and aerodynamic dose emission of indacaterol from a capsule based dry powder inhaler.

Most patients using dry powder inhalers (DPIs) are unable to achieve the inhalation parameters recommended for pharmacopoeial in-vitro dose emission testing. The dose emission characteristics of indacaterol Breezhaler (IB) have been measured using COPD patients' inhalation profiles (IPs) when using IB and replayed in-vitro using a breath simulator attached to an Andersen Cascade Impactor. The peak inhalation flow (PIF) of the profiles ranged from 28.3 to 87.8 L/min and inhaled volumes (Vin) from 0.7 to 3...

Effect of inner pH on peptide acylation within PLGA microspheres.

Polymer degradation within the controlled-release depots comprising of lactide and glycolide (PLGA) forms an acidic microenvironment, in which severe acylation of the peptide by the polymer degradation products takes place. The aim of this study was to make out the role of the inner μpH on peptide acylation within the microspheres and how could it influence the reaction. The effects of pH on the acylation reaction within microspheres were composed of two aspects. Firstly, the inherent effect of pH on the a...

Aryl quinolinyl hydrazone derivatives as anti-inflammatory agents that inhibit TLR4 activation in the macrophages.

A series of aryl 7-chloroquinolinyl hydrazone derivatives (3a-u) have been synthesized in 55-76% yield using simple reaction condition. The synthesized compounds were evaluated for their anti-inflammatory activities based on their ability to inhibit pro-inflammatory cytokine secretion from the macrophages after stimulation with lipopolysaccharide (LPS). Three compounds appeared as promising anti-inflammatory agents. The mechanism of inflammatory activity of the potent compound 3e was further investigated us...

Impact of regional differences along the gastrointestinal tract of healthy adults on oral drug absorption: An UNGAP review.

Oral administration is the most common route of drug delivery. The absorption of a drug from the gut into the bloodstream involves disintegration of the solid dosage form, dissolution of the active pharmaceutical ingredient and its transport across the gut wall. The efficiency of these processes is determined by highly complex and dynamic interplay between the gastrointestinal tract, the dosage form and the API. The European Network on Understanding Gastrointestinal Absorption-related Processes (UNGAP) aims...

High antitumor activity of Sortase A-generated anti-CD20 antibody fragment drug conjugates.

Antibody fragments, as the products of engineered antibodies, exhibit great potential for cancer therapy and imaging. Antibody fragment drug conjugates (AFDCs), which conjugate the highly specific, low-immunity and small-sized antibody fragments with cytotoxic payloads, can overcome the limitations of traditional IgG format drugs in cancer therapy. In this study, a commercialized anti-CD20 monoclonal antibody, ofatumumab (OFA), was applied to generate two site-specific monomethyl auristain E (MMAE)-conjugat...

Effect of electrostatic interactions on the relaxation dynamics of pharmaceutical eutectics.

In this paper, we investigate the temperature dependent relaxation dynamics in the glassy and supercooled liquid state of dipolar and ionic eutectic mixtures made of two anesthetic agents (lidocaine and prilocaine) and their hydrochloride salts, respectively. In addition to eutectic phases containing 1:1 and 4:1 mol/mol of LD/PRL and LD-HCl/PRL-HCl, respectively, the relaxation properties of non-eutectic compositions and parent compounds are also studied. We found that electrostatic long-range forces dete...

Autophagy as a molecular target for cancer treatment.

Autophagy is an evolutionarily conserved catabolic mechanism, by which eukaryotic cells recycle or degrades internal constituents through membrane-trafficking pathway. Thus, autophagy provides the cells with a sustainable source of biomolecules and energy for the maintenance of homeostasis under stressful conditions such as tumor microenvironment. Recent findings revealed a close relationship between autophagy and malignant transformation. However, due to the complex dual role of autophagy in tumor survival...


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