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European Journal of Pharmaceutical Sciences

Klemen Korasa, Franc Vrečer
Over the last two decades, regulatory agencies have demanded better understanding of pharmaceutical products and processes by implementing new technological approaches, such as process analytical technology (PAT). Process analysers present a key PAT tool, which enables effective process monitoring, and thus improved process control of medicinal product manufacturing. Process analysers applicable in pharmaceutical coating unit operations are comprehensibly described in the present article. The review is focused on monitoring of solid oral dosage forms during film coating in two most commonly used coating systems, i...
October 8, 2017: European Journal of Pharmaceutical Sciences
Shreya Thakkar, Dilip Sharma, Manju Misra
INTRODUCTION: Erlotinib is a well known FDA approved drug from category of tyrosine kinase inhibitors; used for the treatment of lung cancer. However its use is limited because of its poor water solubility. OBJECTIVE: The aim of present work was to improve solubility by developing a stable nanocrystal based drug delivery system of ERL with the aid of sodium lauryl sulfate as potential stabilizer and to carry out comparative evaluation of electrospraying and lyophilization as solidification techniques on its solid state properties...
October 6, 2017: European Journal of Pharmaceutical Sciences
Jeremy Perrier, Zhou Zhou, Claire Dunn, Ibrahim Khadra, Clive G Wilson, Gavin Halbert
Upon oral administration the solubility of a drug in intestinal fluid is a key property influencing bioavailability. It is also recognised that simple aqueous solubility does not reflect intestinal solubility and to optimise in vitro investigations simulated intestinal media systems have been developed. Simulated intestinal media which can mimic either the fasted or fed state consists of multiple components each of which either singly or in combination may influence drug solubility, a property that can be investigated by a statistical design of experiment technique...
October 5, 2017: European Journal of Pharmaceutical Sciences
Abimanyu Sugumaran, Chandrasekar Ponnusamy, Palanivel Kandhasamy, Venkateshwaran Krishnaswami, Rajaguru Palanichamy, Ruckmani Kandasamy, Manikandan Lakshmanan, Subramanian Natesan
Targeted delivery of anticancer agents is poised to improve cancer therapy, for which polymers can serve as targeting ligands or nanocarriers for chemotherapeutic agents. In this study, we have developed and evaluated the efficacy of a camptothecin (CPT)-loaded polymer stabilized nanoemulsion (PSNE) for the passive targeted delivery to breast cancer. Based on the pseudo-ternary phase diagrams, PSNEs were developed using capmul MCM:poloxamer 407 (4:1), solutol HS 15:simulsol P23 (1:2) and water. CPT polymer mixture was developed by solvent evaporation technique...
October 5, 2017: European Journal of Pharmaceutical Sciences
Gaia M G Quaroni, Chiara G M Gennari, Francesco Cilurzo, Guylaine Ducouret, Costantino Creton, Paola Minghetti
Eudragit® RL (EuRL) matrices have been proposed to release a drug to the skin. However, no information is available on both viscoelastic and adhesive properties of such compositions. This work focuses on the evaluation of both rheological and texture properties of EuRL differently plasticized with tributyl citrate (TBC) or triacetin (TRI) in order to design a pressure sensitive adhesive suitable for transdermal patch preparation. The patch adhesive properties (i.e. tack, peel adhesion and shear adhesion) as well as its in vitro biopharmaceutical performances were determined after loading ibuprofen, ketoprofen or flurbiprofen...
October 5, 2017: European Journal of Pharmaceutical Sciences
Strahinja Kovačević, Milica Karadžić, Sanja Podunavac-Kuzmanović, Lidija Jevrić
The present study is based on the quantitative structure-activity relationship (QSAR) analysis of binding affinity toward human prion protein (huPrP(C)) of quinacrine, pyridine dicarbonitrile, diphenylthiazole and diphenyloxazole analogs applying different linear and non-linear chemometric regression techniques, including univariate linear regression, multiple linear regression, partial least squares regression and artificial neural networks. The QSAR analysis distinguished molecular lipophilicity as an important factor that contributes to the binding affinity...
October 4, 2017: European Journal of Pharmaceutical Sciences
Aneta Dąbrowska, Michał Matuszewski, Krzysztof Zwoliński, Anna Ignaczak, Agnieszka B Olejniczak
Lipophilicity was investigated for 20 2'-deoxyribonucleoside derivatives modified with electron-neutral 1,2-dicarba-closo-dodecaborane, 1,12-dicarba-closo-dodecaborane, 7,8-dicarba-nido-undecaborate anion, and metallacarborane containing Co, Fe, or Cr. The partition coefficient (P) for neutral conjugates and the distribution coefficient (D7.4) for ionic compounds were determined as a lipophilicity descriptor using a shake-flask method. All modified nucleosides had P/D7.4 values higher than those of an appropriate unmodified 2'-closo-dodecaborane and metallacarborane was found to be three orders of magnitude higher than that of its unmodified counterpart...
October 4, 2017: European Journal of Pharmaceutical Sciences
Mohammad Halayqa, Aneta Pobudkowska, Urszula Domańska, Maciej Zawadzki
Synthesis of three mefenamic acid (MEF) derivatives - ionic liquid compounds composed of MEF in an anionic form and ammonium cation (choline, MEF1), or {di(2-hydroxyethyl)dimethyl ammonium (MEF2)}, or {tri(2-hydroxyethyl)methyl ammonium compound (MEF3)} is presented. The basic thermal properties of pure compounds i.e. fusion temperatures, and the enthalpy of fusion of these compounds have been measured with differential scanning microcalorimetry technique (DSC). Molar volumes have been calculated with the Barton group contribution method...
October 3, 2017: European Journal of Pharmaceutical Sciences
Cecilie Maria Madsen, Kung-I Feng, Andrew Leithead, Nicole Canfield, Søren Astrup Jørgensen, Anette Müllertz, Thomas Rades
The composition of the human intestinal fluids varies both intra- and inter-individually. This will influence the solubility of orally administered drug compounds, and hence, the absorption and efficacy of compounds displaying solubility limited absorption. The purpose of this study was to assess the influence of simulated intestinal fluid (SIF) composition on the solubility of poorly soluble compounds. Using a Design of Experiments (DoE) approach, a set of 24 SIF was defined within the known compositions of human fasted state intestinal fluid...
October 3, 2017: European Journal of Pharmaceutical Sciences
Franklin C Kenechukwu, Anthony A Attama, Emmanuel C Ibezim, Petra O Nnamani, Chukwuebuka E Umeyor, Emmanuel M Uronnachi, Thaddeus H Gugu, Mumuni A Momoh, Kenneth C Ofokansi, Paul A Akpa
The use of conventional vaginal formulations of miconazole nitrate (MN) in the treatment of deep-seated VVC (vulvovaginal candidiasis) is limited by poor penetration capacity and low solubility of MN, short residence time and irritation at the application site. Surface-modified mucoadhesive microgels were developed to minimize local irritation, enhance penetration capacity and solubility and prolong localized vaginal delivery of MN for effective treatment of deep-seated VVC. Solid lipid microparticles (SLMs) were prepared from matrices consisting of hydrogenated palm oil (Softisan® 154, SF) and super-refined sunseed oil (SO) with or without polyethylene glycol (PEG)-4000, characterized for physicochemical performance and used to prepare mucoadhesive microgels (MMs) encapsulating MN, employing Polycarbophil as bioadhesive polymer...
October 3, 2017: European Journal of Pharmaceutical Sciences
Qingliang Yang, Yingliang Ma, Jesse Zhu
Dry powder coated osmotic drug delivery system (ODDS) were prepared and characterized using an innovative powder coating technology. Coating powder adhesion to the surface of the ODDS core was firstly performed through an electrostatic spray gun, followed by a curing step to allow those electrically deposited particles coalesce and form a continuous, uniform and strong coating film, which is the semipermeable membrane of the ODDS. Triethyl citrate (TEC) was found to be a better liquid plasticizer than PEG 400 both in reducing the glass transition temperature of the coating polymer (cellulose acetate) and in increasing the electrical conductivity of the ODDS cores, both of which led to an enhanced coating powder adhesion and film formation...
October 3, 2017: European Journal of Pharmaceutical Sciences
Aditya Darade, Sulabha Pathak, Shobhona Sharma, Vandana Patravale
Atovaquone in combination with proguanil hydrochloride, marketed as Malarone® tablets by GlaxoSmithKline (GSK), is prescribed for the treatment of malaria. High dose and poor bioavailability are the main hurdles associated with atovaquone oral therapy. The present study reports development of atovaquone nanoparticles, using in house designed and fabricated electrospraying equipment, and the assessment of bioavailability and therapeutic efficacy of the nanoparticles after oral administration. Solid nanoparticles of atovaquone were successfully produced by electrospraying and were characterized for particle size and flow properties...
September 30, 2017: European Journal of Pharmaceutical Sciences
Laetitia Minh Mai Lê, Marion Berge, Ali Tfayli, Jiangyan Zhou, Patrice Prognon, Arlette Baillet-Guffroy, Eric Caudron
The aim of this study was to assess the ability of Raman spectroscopy to discriminate and quantify five antineoplastic drugs in an aqueous matrix at low concentrations before patient administration. Five antineoplastic drugs were studied at therapeutic concentrations in aqueous 0.9% sodium chloride: 5-fluorouracil (5FU), gemcitabine (GEM), cyclophophamide (CYCLO), ifosfamide (IFOS) and doxorubicin (DOXO). All samples were packaged in glass vials and analyzed using Raman spectrometry from 400 to 4000cm(-1). Discriminant analyses were performed using Partial Least Squares Discriminant Analysis (PLS-DA) and quantitative analyses using PLS regression...
September 29, 2017: European Journal of Pharmaceutical Sciences
Vincent Jannin, Lucia Blas, Stéphanie Chevrier, Cédric Miolane, Frédéric Demarne, Denis Spitzer
OBJECTIVE: To evaluate the digestibility of Solid Lipid Nanoparticles (SLN) of glyceryl dibehenate prepared either with surfactants by ultrasonication or without surfactant by spray-flash evaporation. METHODS: SLN of glyceryl dibehenate (Compritol® 888 ATO) were produced by two processes: (i) high-shear homogenization with a solution of water-soluble surfactants followed by ultrasonication (ii) and Spray-Flash Evaporation (SFE) of the pure lipid. The digestibility of these nanoparticles was then tested by in vitro lipolysis using a pH-stat apparatus and the assay of glycerides by gel phase chromatography...
September 29, 2017: European Journal of Pharmaceutical Sciences
Alessandro Venuta, Francesca Moret, Giovanni Dal Poggetto, Diletta Esposito, Aurore Fraix, Concetta Avitabile, Francesca Ungaro, Mario Malinconico, Salvatore Sortino, Alessandra Romanelli, Paola Laurienzo, Elena Reddi, Fabiana Quaglia
Polymeric nanoparticles (NPs) of poly(ε-caprolactone) (PCL) covered with a hydrophilic poly(ethylene glycol) (PEG) shell are usually prepared from diblock PEG-PCL copolymers through different techniques. Furthermore PEG, NPs can be decorated with targeting ligands to accumulate in specific cell lines. However, the density and conformation of PEG on the surface and its impact on the exposition of small targeting ligands has been poorly considered so far although this has a huge impact on biological behaviour...
September 28, 2017: European Journal of Pharmaceutical Sciences
Tijia Chen, Ting Gong, Ting Zhao, Yao Fu, Zhirong Zhang, Tao Gong
To achieve tumor-selective drug delivery, various nanocarriers have been explored using either passive or active targeting strategies. Despite the great number of studies published annually in the field, only nanocarriers using approved excipients reach the clinical stage. In our study, two classic nanoscale formulations, nanoemulsion (NE) and liposome (Lipo) were selected for the encapsulation of lycobetaine (LBT). To improve the lipid solubility of LBT, oleic acid (OA) was used to complex (LBT-OA) with lycobetaine (LBT)...
September 28, 2017: European Journal of Pharmaceutical Sciences
Tomohiro Yoshida, Tatsuki Fukami, Takaya Kurokawa, Saki Gotoh, Akifumi Oda, Miki Nakajima
Carboxylesterase (CES) and arylacetamide deacetylase (AADAC) are the major enzymes responsible for the hydrolysis of various clinical drugs. Our recent study demonstrated that the identity of the responsible hydrolase can be roughly surmised based on the chemical structures of compounds in humans. Dogs are used for preclinical studies in drug development, but the substrate specificities of dog CES and AADAC remain to be clarified. The purpose of this study is to characterize their substrate specificities. We prepared recombinant dog CES1, CES2, and AADAC...
September 28, 2017: European Journal of Pharmaceutical Sciences
Mailine Gehrcke, Marcel Henrique Marcondes Sari, Luana Mota Ferreira, Allanna Valentini Barbieri, Laura Minussi Giuliani, Vinicius Costa Prado, Jessica Mendes Nadal, Paulo Vitor Farago, Cristina Wayne Nogueira, Letícia Cruz
This study aimed the development of nanocapsules (NCs) for oral indole-3-carbinol (I3C) administration and evaluation of antinociceptive potential of this compound in its two forms, free and nanoencapsulated, using acute pain models. NCs showed adequate physicochemical characteristics and protected the I3C against UVC radiation exposure. It was observed no chemical bond between I3C and polymer by FTIR. Besides, X-ray and DSC analysis suggested that I3C was molecularly dispersed in NCs. The dialysis bag technique showed that almost 100% of the compound was released from NCs at 360min...
September 28, 2017: European Journal of Pharmaceutical Sciences
Eman Gomaa, Amr S Abu Lila, Azza A Hasan, Fakhr-Eldin S Ghazy
Vaginal route has been recently considered as a potential route for systemic delivery of drugs with poor oral bioavailability. Vardenafil (VDF) is a relatively new phosphodiesterase-5 inhibitor that exhibits a limited oral bioavailability (≈15%) due to extensive first-pass metabolism. In this study, we attempted to enhance the systemic bioavailability of VDF via its formulation within vaginal suppositories. Witepsol H15 and Suppocire NA50 were adopted as lipophilic suppository bases while polyethylene glycol 4000/400 and glycerogelatin were used as hydrophilic suppository bases...
September 28, 2017: European Journal of Pharmaceutical Sciences
Yunning Yang, Yuting Guo, Xinyi Tan, Haibing He, Yu Zhang, Tian Yin, Hui Xu, Xing Tang
In the present study, vincristine (VCR)-loaded liposomes were designed by ion-pairing techniques and the model could be applied to investigate the effect of lipids on the degradation of vinca alkaloids, and how to weaken their influence by adjusting pH and adding antioxidants. It was found that there was a positive correlation between degree of degradation and the unsaturation extent of the phospholipids. In the phospholipid with the lowest oxidation index, only 6% of VCR was degraded in 6days at 37°C, whereas for the phospholipids with highest oxidation index, the degradation reached above 95% over the same time...
September 28, 2017: European Journal of Pharmaceutical Sciences
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