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Pharmaceutics

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https://read.qxmd.com/read/30781728/mono-and-bi-phasic-cellulose-acetate-micro-vectors-for-anti-inflammatory-drug-delivery
#1
Vincenzo Guarino, Rosaria Altobelli, Tania Caputo, Luigi Ambrosio, Sergio Caserta, Paola Calcagnile, Christian Demitri
In recent years, different processing technologies have been engineered to fabricate capsules or particles with peculiar properties (e.g., swelling, pH-sensitive response) at the micro and sub-micrometric size scale, to be used as carriers for controlled drug and molecular release. Herein, the development of cellulose acetate (CA) micro-carriers with mono- (MC) or bi-phasic (BC) composition is proposed, fabricated via electrohydrodynamic atomization (EHDA)-an electro-dropping technology able to micro-size polymer solution by the application of high voltage electrostatic forces...
February 18, 2019: Pharmaceutics
https://read.qxmd.com/read/30781722/chitosan-coated-nanoparticles-effect-of-chitosan-molecular-weight-on-nasal-transmucosal-delivery
#2
Franciele Aline Bruinsmann, Stefania Pigana, Tanira Aguirre, Gabriele Dadalt Souto, Gabriela Garrastazu Pereira, Annalisa Bianchera, Laura Tiozzo Fasiolo, Gaia Colombo, Magno Marques, Adriana Raffin Pohlmann, Silvia Stanisçuaski Guterres, Fabio Sonvico
Drug delivery to the brain represents a challenge, especially in the therapy of central nervous system malignancies. Simvastatin (SVT), as with other statins, has shown potential anticancer properties that are difficult to exploit in the central nervous system (CNS). In the present work the physico⁻chemical, mucoadhesive, and permeability-enhancing properties of simvastatin-loaded poly-ε-caprolactone nanocapsules coated with chitosan for nose-to-brain administration were investigated. Lipid-core nanocapsules coated with chitosan (LNCchit ) of different molecular weight (MW) were prepared by a novel one-pot technique, and characterized for particle size, surface charge, particle number density, morphology, drug encapsulation efficiency, interaction between surface nanocapsules with mucin, drug release, and permeability across two nasal mucosa models...
February 18, 2019: Pharmaceutics
https://read.qxmd.com/read/30781585/nanoemulsions-for-nose-to-brain-drug-delivery
#3
REVIEW
Maria Cristina Bonferoni, Silvia Rossi, Giuseppina Sandri, Franca Ferrari, Elisabetta Gavini, Giovanna Rassu, Paolo Giunchedi
The blood⁻brain barrier (BBB) plays a fundamental role in protecting the brain from toxic substances and therefore also controls and restricts the entry of therapeutic agents. The nasal administration of drugs using the nose-to-brain pathway allows direct drug targeting into the brain, avoiding the first-pass effect and bypassing the BBB. Through the nasal route, the drug can access the brain directly along the trigeminal and olfactory nerves, which are located in the upper part of the nasal cavity. Nanoemulsions are formulations belonging to the field of nanomedicine...
February 17, 2019: Pharmaceutics
https://read.qxmd.com/read/30781584/1-4-dihydropyridine-antihypertensive-drugs-recent-advances-in-photostabilization-strategies
#4
REVIEW
Michele De Luca, Giuseppina Ioele, Gaetano Ragno
The 1,4-dihydropyridine (DHP) drugs are nowadays the most used drugs in the treatment of hypertension. However, all the structures in this series present a significant sensitivity to light, leading to the complete loss of pharmacological activity. This degradation is particularly evident in aqueous solution, so much so that almost all DHP drugs on the market are formulated in solid preparations, especially tablets. The first and main process of photodegradation consists in the aromatization of the dihydropyridine ring, after which secondary processes can take place on the various substituents...
February 17, 2019: Pharmaceutics
https://read.qxmd.com/read/30781442/potential-use-of-the-maillard-reaction-for-pharmaceutical-applications-gastric-and-intestinal-controlled-release-alginate-albumin-beads
#5
Mouhamad Khoder, Henry K Gbormoi, Ali Ryan, Ayman Karam, Raid G Alany
In this study, bovine serum albumin (BSA) and alginate (ALG) conjugates were synthesized by the Maillard reaction in order to evaluate their potential to develop controlled release drug delivery systems. The progress of the Maillard reaction was evidenced using ultraviolet (UV) absorbance, determination of BSA remaining free amino groups, and sodium dodecyl sulfate polyacrylamide gel electrophoresis (SDS-PAGE). BSA-ALG conjugates possessed enhanced and tunable viscosity, foamability and foam stability. Foam generated from BSA-ALG conjugate solution was used to prepare floating gastroretentive calcium ALG beads...
February 15, 2019: Pharmaceutics
https://read.qxmd.com/read/30781383/design-and-evaluation-of-an-extended-release-olmesartan-tablet-using-chitosan-cyclodextrin-composites
#6
Makoto Anraku, Ryo Tabuchi, Miwa Goto, Daisuke Iohara, Yasuyuki Mizukai, Yuji Maezaki, Akihiro Michihara, Daisuke Kadowaki, Masaki Otagiri, Fumitoshi Hirayama
Sustained-release olmesartan tablets (OLM) were prepared by the simple, direct compression of composites of anionic sulfobutyl ether-β-cyclodextrin (SBE-β-CD) and cationic spray-dried chitosan (SD-CS), and were evaluated for use as a sustained release preparation for the treatment of hypertension. An investigation of the interaction between OLM and SBE-β-CD by the solubility method indicated that the phase diagram of the OLM/SBE-β-CD system was the AL type, indicating the formation of a 1:1 inclusion complex...
February 15, 2019: Pharmaceutics
https://read.qxmd.com/read/30769938/a-review-on-hydro-porphyrin-loaded-polymer-micelles-interesting-and-valuable-platforms-for-enhanced-cancer-nanotheranostics
#7
REVIEW
Bruno F O Nascimento, Nelson A M Pereira, Artur J M Valente, Teresa M V D Pinho E Melo, Marta Pineiro
Porphyrins are known therapeutic agents for photodynamic therapy of cancer and also imaging agents for NIR fluorescence imaging, MRI, or PET. A combination of interesting features makes tetrapyrrolic macrocycles suitable for use as theranostic agents whose full potential can be achieved using nanocarriers. This review provides an overview on nanotheranostic agents based on polymeric micelles and porphyrins developed so far.
February 15, 2019: Pharmaceutics
https://read.qxmd.com/read/30769846/polymer-distribution-and-mechanism-conversion-in-multiple-media-of-phase-separated-controlled-release-film-coating
#8
Lu Chen, Guobao Yang, Xiaoyang Chu, Chunhong Gao, Yuli Wang, Wei Gong, Zhiping Li, Yang Yang, Meiyan Yang, Chunsheng Gao
Phase-separated films of water-insoluble ethyl cellulose (EC) and water-soluble hydroxypropyl cellulose (HPC) can be utilized to tailor drug release from coated pellets. In the present study, the effects of HPC levels and the pH, type, ionic strength and osmolarity of the media on the release profiles of soluble metoprolol succinates from the EC/HPC-coated pellets were investigated, and the differences in drug-release kinetics in multiple media were further elucidated through the HPC leaching and swelling kinetics of the pellets, morphology (SEM) and water uptake of the free films and the interaction between the coating polymers and the media compositions...
February 14, 2019: Pharmaceutics
https://read.qxmd.com/read/30781880/multivariate-statistical-optimization-of-tablet-formulations-incorporating-high-doses-of-a-dry-herbal-extract
#9
Euichaul Oh, Uijung Kim, Beom-Jin Lee, Cheol Moon
The development of oral tablet formulation for herbal medicines has been restricted by large drug loadings and the poor physicochemical and mechanical properties of dry herbal extracts (DHEs). Herein, statistical experimental designs were applied to herbal tablet formulation development and optimization using Wuzi Yanzong dry extract (WYE). The tablet disintegration time and hardness were identified as the critical quality attributes (CQAs) of the product. The tablet formulation was designed to achieve a high drug loading (50% or higher of WYE), shorter tablet disintegration time (less than 30 minutes), and suitable hardness (6...
February 13, 2019: Pharmaceutics
https://read.qxmd.com/read/30781867/intestinal-permeation-enhancers-for-oral-delivery-of-macromolecules-a-comparison-between-salcaprozate-sodium-snac-and-sodium-caprate-c-10
#10
REVIEW
Caroline Twarog, Sarinj Fattah, Joanne Heade, Sam Maher, Elias Fattal, David J Brayden
Salcaprozate sodium (SNAC) and sodium caprate (C10 ) are two of the most advanced intestinal permeation enhancers (PEs) that have been tested in clinical trials for oral delivery of macromolecules. Their effects on intestinal epithelia were studied for over 30 years, yet there is still debate over their mechanisms of action. C10 acts via openings of epithelial tight junctions and/or membrane perturbation, while for decades SNAC was thought to increase passive transcellular permeation across small intestinal epithelia based on increased lipophilicity arising from non-covalent macromolecule complexation...
February 13, 2019: Pharmaceutics
https://read.qxmd.com/read/30781850/mesoporous-silica-nanomaterials-versatile-nanocarriers-for-cancer-theranostics-and-drug-and-gene-delivery
#11
REVIEW
Samuel Kesse, Kofi Oti Boakye-Yiadom, Belynda Owoya Ochete, Yaw Opoku-Damoah, Fahad Akhtar, Mensura Sied Filli, Muhammad Asim Farooq, Md Aquib, Bazezy Joelle Maviah Mily, Ghulam Murtaza, Bo Wang
Mesoporous silica nanomaterials (MSNs) have made remarkable achievements and are being thought of by researchers as materials that can be used to effect great change in cancer therapies, gene delivery, and drug delivery because of their optically transparent properties, flexible size, functional surface, low toxicity profile, and very good drug loading competence. Mesoporous silica nanoparticles (MSNPs) show a very high loading capacity for therapeutic agents. It is well known that cancer is one of the most severe known medical conditions, characterized by cells that grow and spread rapidly...
February 13, 2019: Pharmaceutics
https://read.qxmd.com/read/30759886/improved-morphine-loaded-hydrogels-for-wound-related-pain-relief
#12
Dinis Mateus, Joana Marto, Patrícia Trindade, Humberto Gonçalves, Ana Salgado, Paula Machado, António Melo-Gouveia, Helena M Ribeiro, António J Almeida
The use of morphine applied topically to painful wounds has potential advantages, such as dose reduction, fewer side effects and compound formulations, have been proposed for this purpose. Given the potential high impact of drug product quality on a patient's health, the aim of the present study was to develop two stable sterile hydrogels containing morphine hydrochloride, intended for topical application on painful wounds. Two carboxymethylcellulose sodium-based hydrogels were prepared containing 0.125% w / w (F1-MH semi-solid formulation) and 1...
February 12, 2019: Pharmaceutics
https://read.qxmd.com/read/30759879/investigation-of-the-quantity-of-exhaled-aerosols-released-into-the-environment-during-nebulisation
#13
James A McGrath, Andrew O'Sullivan, Gavin Bennett, Ciarraí O'Toole, Mary Joyce, Miriam A Byrne, Ronan MacLoughlin
BACKGROUND: Secondary inhalation of medical aerosols is a significant occupational hazard in both clinical and homecare settings. Exposure to fugitive emissions generated during aerosol therapy increases the risk of the unnecessary inhalation of medication, as well as toxic side effects. METHODS: This study examines fugitively-emitted aerosol emissions when nebulising albuterol sulphate, as a tracer aerosol, using two commercially available nebulisers in combination with an open or valved facemask or using a mouthpiece with and without a filter on the exhalation port...
February 12, 2019: Pharmaceutics
https://read.qxmd.com/read/30744157/effect-of-carrier-lipophilicity-and-preparation-method-on-the-properties-of-andrographolide%C3%A2-solid-dispersion
#14
Guowei Zhao, Qingyun Zeng, Shoude Zhang, Youquan Zhong, Changhao Wang, Yashao Chen, Liquan Ou, Zhenggen Liao
Solid dispersion (SD) is a useful approach to improve the dissolution rate and bioavailability of poorly water-soluble drugs. This work investigated the effects of carrier material lipophilicity and preparation method on the properties of andrographolide (AG)⁻SD. The SDs of AG and the carrier materials, polyethylene glycol (PEG) and PEG grafted with carbon chains of different length (grafted PEG), have been prepared by spray-drying and vacuum-drying methods. In AG⁻SDs prepared by the different preparation methods with the same polymer as carrier material, the intermolecular interaction, 5% weight-loss temperature, the melting temperature (Tm ), surface morphology, crystallinity, and dissolution behavior have significant differences...
February 10, 2019: Pharmaceutics
https://read.qxmd.com/read/30744154/dual-action-of-the-pn159-klal-map-peptide-increase-of-drug-penetration-across-caco-2-intestinal-barrier-model-by-modulation-of-tight-junctions-and-plasma-membrane-permeability
#15
Alexandra Bocsik, Ilona Gróf, Lóránd Kiss, Ferenc Ötvös, Ottó Zsíros, Lejla Daruka, Lívia Fülöp, Monika Vastag, Ágnes Kittel, Norbert Imre, Tamás A Martinek, Csaba Pál, Piroska Szabó-Révész, Mária A Deli
The absorption of drugs is limited by the epithelial barriers of the gastrointestinal tract. One of the strategies to improve drug delivery is the modulation of barrier function by the targeted opening of epithelial tight junctions. In our previous study the 18-mer amphiphilic PN159 peptide was found to be an effective tight junction modulator on intestinal epithelial and blood⁻brain barrier models. PN159, also known as KLAL or MAP, was described to interact with biological membranes as a cell-penetrating peptide...
February 10, 2019: Pharmaceutics
https://read.qxmd.com/read/30744102/chitosan-plus-compound-48-80-formulation-and-preliminary-evaluation-as-a-hepatitis-b-vaccine-adjuvant
#16
Dulce Bento, Sandra Jesus, Filipa Lebre, Teresa Gonçalves, Olga Borges
Current vaccine research is mostly based on subunit antigens. Despite the better toxicity profile of these antigens they are often poorly immunogenic, so adjuvant association has been explored as a strategy to obtain a potent vaccine formulation. Recently, mast cell activators were recognized as a new class of vaccine adjuvants capable of potentiating mucosal and systemic immune responses. In this study, a co-adjuvanted delivery system was developed and characterized, combining the mast cell activator C48/80 with chitosan nanoparticles (Chi-C48/80 NPs), and the results were compared with plain chitosan nanoparticles...
February 9, 2019: Pharmaceutics
https://read.qxmd.com/read/30736486/hybrid-nanogels-stealth-and-biocompatible-structures-for-drug-delivery-applications
#17
REVIEW
Parisa Eslami, Filippo Rossi, Stefano Fedeli
Considering nanogels, we have focused our attention on hybrid nanosystems for drug delivery and biomedical purposes. The distinctive strength of these structures is the capability to join the properties of nanosystems with the polymeric structures, where versatility is strongly demanded for biomedical applications. Alongside with the therapeutic effect, a non-secondary requirement of the nanosystem is indeed its biocompatibility. The importance to fulfill this aim is not only driven by the priority to reduce, as much as possible, the inflammatory or the immune response of the organism, but also by the need to improve circulation lifetime, biodistribution, and bioavailability of the carried drugs...
February 7, 2019: Pharmaceutics
https://read.qxmd.com/read/30736430/applicability-of-a-modified-rat-model-of-acute-arthritis-for-long-term-testing-of-drug-delivery-systems
#18
Imke Rudnik-Jansen, Nina Woike, Suzanne de Jong, Sabine Versteeg, Marja Kik, Pieter Emans, George Mihov, Jens Thies, Niels Eijkelkamp, Marianna Tryfonidou, Laura Creemers
Episodes of inflammation and pain are predominant features of arthritic joint diseases. Drug delivery systems (DDS) could reduce inflammation and pain long-term without chances of infection upon multiple injections. To allow for long-term evaluation of DDS, we modified a previously published acute arthritis model by extending follow-up periods between flare-ups. Unilateral synovial inflammation of the knee was induced by intra-articular injection of streptococcal cell wall peptidoglycan polysaccharide (PGPS), and flare-ups were induced by intravenous PGPS injections every 4 weeks for a total duration of 84 days...
February 7, 2019: Pharmaceutics
https://read.qxmd.com/read/30736367/preparation-and-characterization-of-new-liposomes-bactericidal-activity-of-cefepime-encapsulated-into-cationic-liposomes
#19
Maria Luisa Moyá, Manuel López-López, José Antonio Lebrón, Francisco José Ostos, David Pérez, Vanesa Camacho, Irene Beck, Vicente Merino-Bohórquez, Manuel Camean, Nuria Madinabeitia, Pilar López-Cornejo
Cefepime is an antibiotic with a broad spectrum of antimicrobial activity. However, this antibiotic has several side effects and a high degradation rate. For this reason, the preparation and characterization of new liposomes that are able to encapsulate this antibiotic seem to be an important research line in the pharmaceutical industry. Anionic and cationic liposomes were prepared and characterized. All cationic structures contained the same cationic surfactant, N , N , N -triethyl- N -(12-naphthoxydodecyl)ammonium...
February 6, 2019: Pharmaceutics
https://read.qxmd.com/read/30736357/amorphisation-of-free-acid-ibuprofen-and-other-profens-in-mixtures-with-nanocellulose-dry-powder-formulation-strategy-for-enhanced-solubility
#20
Athanasios Mantas, Valentine Labbe, Irena Loryan, Albert Mihranyan
The formulation of arylpropionic acid derivatives (profens), which are poorly soluble Biopharmaceutical Classification System (BCS) Type II drugs, has a strong impact on their therapeutic action. This article shows that heat-treated powder mixtures of free acid profens with high surface area Cladophora cellulose induces drug amorphization and results in enhanced solubility and bioavailability. Similar mixtures produced using conventional low surface area cellulose, i.e., microcrystalline cellulose, does not produce the same effect...
February 6, 2019: Pharmaceutics
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