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A novel approach for dry powder coating of pellets with Ethylcellulose. Part I: Evaluation of film formulation and process set up
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Beatrice Albertini, Serena Bertoni, Cecilia Melegari, Luisa Stella Dolci, Nadia Passerini An innovative dry powder coating technology was developed in a high-shear granulator using ethylcellulose (E10) as polymer. Several solid plasticizers were investigated with the aim of decreasing the polymer Tg at least to the highest possible working temperature (80°C). DSC analysis of physical mixtures of E10 and plasticizers evidenced that lauric acid (LA) was the most effective plasticizer. In order to reac...
Source: International Journal of Pharmaceutics - November 30, 2016 Category: Drugs & Pharmacology Source Type: research

Preparation, characterization and in vivo pharmacokinetic study of PVP-modified oleanolic acid liposomes
Publication date: 30 January 2017 Source:International Journal of Pharmaceutics, Volume 517, Issues 1–2 Author(s): Yan Liu, Xiao Luo, Xiaochao Xu, Nannan Gao, Xiaohong Liu The primary purpose of the present study was to design and optimize a liposomal formulation of the poorly water-soluble drug oleanolic acid (OA) to improve its oral bioavailability, and prolong the duration of therapeutic drug level. Liposomes containing a soybean lecithin and cholesterol lipid bilayer, a protective hydrophilic polyvinylpyrrolidone-K30 (PVP-K30) coating, and a protective bile salt, sodium deoxycholate, were prepared by a thin-film...
Source: International Journal of Pharmaceutics - November 30, 2016 Category: Drugs & Pharmacology Source Type: research

Solid lipid nanoparticles for sustained pulmonary delivery of Yuxingcao essential oil: Preparation, characterization and in vivo evaluation
The objective of this study was to prepare solid lipid nanoparticles (SLNs) for sustained pulmonary delivery of Yuxingcao essential oil (YEO). Three YEO loaded SLNs (SLN-200, SLN-400 and SLN-800) with different particle size were prepared and separated following a high-shear homogenization technique using Compritol 888 ATO as lipid and polyvinyl alcohol as an emulsifier. The particle size, zeta potential, drug encapsulation efficiency and drug loading of the SLNs were determined to be between 171 and 812nm, −17.1 and −19.3mV, between 76.6 and 90.2% and between 2.34 and 3.12%, respectively whereas the in vitro r...
Source: International Journal of Pharmaceutics - November 29, 2016 Category: Drugs & Pharmacology Source Type: research

Calcium phosphate nanoparticles functionalized with alendronate-conjugated polyethylene glycol (PEG) for the treatment of bone metastasis
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Weijing Chu, Yanjuan Huang, Chanzhen Yang, Yunhui Liao, Xuefei Zhang, Mina Yan, Shengmiao Cui, Chunshun Zhao Because of the peculiarity of the bone microstructure, the uptake of chemotherapeutics often happens at non-targeted sites, which induces side effects. In order to solve this problem, we designed a bone-targeting drug delivery system that can release drug exclusively in the nidus of the bone. Alendronate (ALN), which has a high ability to target to hydroxyapatite, was used to fabricate double ALN...
Source: International Journal of Pharmaceutics - November 29, 2016 Category: Drugs & Pharmacology Source Type: research

Pharmaceutical technology can turn a traditional drug, dexamethasone into a first-line ocular medicine. A global perspective and future trends
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Javier Rodríguez Villanueva, Laura Rodríguez Villanueva, Manuel Guzmán Navarro Dexamethasone is one of the most prescribed glucocorticoids. It is effective and safe in the treatment of a wide variety of ocular conditions, including anterior and posterior segment inflammation. However, its half-life in the vitreous humor is very short, which means that it typically requires frequent administrations, thus reducing patient adherence and causing therapeutic failure. Innovative dexametha...
Source: International Journal of Pharmaceutics - November 28, 2016 Category: Drugs & Pharmacology Source Type: research

Surfactant effect on the physicochemical characteristics of cationic solid lipid nanoparticles
In this study, three different cationic lipids (dioctadecyl dimethyl ammonium bromide, cetyltrimethyl ammonium bromide, cetylpyridinium chloride) and Brij 76 as nonionic surfactant were employed to formulate Precirol ATO 5 based cSLN using pEGFP-LUC as model plasmid. The physicochemical properties of cSLN were influenced by both type and amount of surfactants. Thermal analyses of bulk cSLN showed endothermic peaks significantly different from the ones of the single pure components, hinting a complete entanglement of the lipid matrix with the surfactants and justifying the different behavior of the cSLN in the ability to in...
Source: International Journal of Pharmaceutics - November 27, 2016 Category: Drugs & Pharmacology Source Type: research

pH-Sensitive PEGylated liposomes for delivery of an acidic dinitrobenzamide mustard prodrug: Pathways of internalization, cellular trafficking and cytotoxicity to cancer cells
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Mimi M. Yang, William R. Wilson, Zimei Wu This paper aims to develop and evaluate a pH-sensitive PEGylated liposomal (pPSL) system for tumor-targeted intracellular delivery of SN25860, a weakly acidic, poorly water-soluble dinitrobenzamide mustard prodrug which is activated by the E. coli nitroreductase nfB. pPSL and non pH-sensitive liposomes (nPSL), as reference, were formulated by thin-film hydration; an active drug loading method was developed with the aid of solubilizers. Cytotoxicity was evaluated...
Source: International Journal of Pharmaceutics - November 27, 2016 Category: Drugs & Pharmacology Source Type: research

Polyethylenimine-functionalized carbon nanotubes tagged with AS1411 aptamer for combination gene and drug delivery into human gastric cancer cells
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Sahar Taghavi, Azadeh Hashem Nia, Khalil Abnous, Mohammad Ramezani In this project, synergistic cancer cell death was achieved by a targeted delivery system comprising Bcl-xL-specific shRNA and a very low DOX content, which simultaneously activated an intrinsic apoptotic pathway. A modified branched polyethylenimine (PEI 10kDa) was grafted through polyethylene glycol (PEG) linker to carboxylated single-walled carbon nanotubes (SWCNT) to serve as a vehicle for shRNA delivery. The SWNT-PEG-PEI conjugate w...
Source: International Journal of Pharmaceutics - November 27, 2016 Category: Drugs & Pharmacology Source Type: research

Paclitaxel-loaded polymeric nanoparticles combined with chronomodulated chemotherapy on lung cancer: In vitro and in vivo evaluation
The objective of our study was to examine the anti-tumor effect of paclitaxel (PTX)-loaded polymeric nanoparticles (PTX-NPs) combined with circadian chronomodulated chemotherapy. Our intention was to screen out the best time of the day for the drug to be administered. PTX-NPs with a diameter of approximately 168nm were prepared through a thin film dispersion technique. The PTX in PTX-NPs showed an initial fast release subsequently a slower and sustained release. The cytotoxicity of chronomodulated administration of PTX-NPs in vitro confirmed that its cytotoxic effect was lower than that of PTX injection, and showed a time-...
Source: International Journal of Pharmaceutics - November 24, 2016 Category: Drugs & Pharmacology Source Type: research

Needleless coaxial electrospinning: A novel approach to mass production of coaxial nanofibers
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Lucie Vysloužilová, Matej Buzgo, Pavel Pokorný, Jiří Chvojka, Andrea Míčková, Michala Rampichová, Jiří Kula, Karel Pejchar, Martin Bílek, David Lukáš, Evžen Amler Herein, we describe a simple spinneret setup for needleless coaxial electrospinning that exceeds the limited production capacity of current approaches. The proposed weir spinneret enables coaxial electrospinning from free liquid surface. This approach leads to the forma...
Source: International Journal of Pharmaceutics - November 24, 2016 Category: Drugs & Pharmacology Source Type: research

Development of flexible nanocarriers for siRNA delivery into tumor tissue
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Hyunkyung Jung, Yuri Shimatani, Mahadi Hasan, Kohei Uno, Susumu Hama, Kentaro Kogure Various non-viral delivery systems for small interfering RNAs (siRNA) have been developed. Such delivery systems generally exhibit tightly formed spherical structures. While such carriers have demonstrated good transfection activity in mono-layered cell systems, effects against solid tumors are often less apparent and difficult to demonstrate, likely due to the rigid structures of the carriers, which may prevent penetra...
Source: International Journal of Pharmaceutics - November 24, 2016 Category: Drugs & Pharmacology Source Type: research

γ-Cyclodextrin
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Phennapha Saokham, Thorsteinn Loftsson γ-Cyclodextrin (γCD) is a cyclic oligosaccharide formed by bacterial digestion of starch and used as solubilizing agent and stabilizer in a variety of pharmaceutical and food products. γCD is a large (molecular weight 1297Da) hydrophilic molecule that does not readily permeate biological membranes and is rapidly digested by bacteria in the gastrointestinal tract. In humans γCD is metabolized by α-amylase that is found in, for example, ...
Source: International Journal of Pharmaceutics - November 24, 2016 Category: Drugs & Pharmacology Source Type: research

Application of DoE approach in the development of mini-capsules, based on biopolymers and manuka honey polar fraction, as powder formulation for the treatment of skin ulcers
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Marika Tenci, Silvia Rossi, Maria Cristina Bonferoni, Giuseppina Sandri, Irene Mentori, Cinzia Boselli, Antonia Icaro Cornaglia, Maria Daglia, Anna Marchese, Carla Caramella, Franca Ferrari The aim of the present work was the development of a powder formulation for the delivery of manuka honey (MH) bioactive components in the treatment of chronic skin ulcers. In particular pectin (PEC)/chitosan glutamate (CS)/hyaluronic acid (HA) mini-capsules were obtained by inverse ionotropic gelation in presence of ...
Source: International Journal of Pharmaceutics - November 24, 2016 Category: Drugs & Pharmacology Source Type: research

Spherical agglomerates of lactose with enhanced mechanical properties
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Dejan Lamešić, Odon Planinšek, Zoran Lavrič, Ilija Ilić The aim of this study was to prepare spherical agglomerates of lactose and to evaluate their physicochemical properties, flow properties, particle friability and compaction properties, and to compare them to commercially available types of lactose for direct compression (spray-dried, granulated and anhydrous β-lactose). Porous spherical agglomerates of α-lactose monohydrate with radially arranged prism-like primary parti...
Source: International Journal of Pharmaceutics - November 22, 2016 Category: Drugs & Pharmacology Source Type: research

Microencapsulated SLN: An innovative strategy for pulmonary protein delivery
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Diana P Gaspar, Carmen Serra, Paulo R Lino, Lídia Gonçalves, Pablo Taboada, Carmen Remuñán-López, António J Almeida Associating protein with nanoparticles is an interesting strategy to improve their bioavailability and biological activity. Solid lipid nanoparticles (SLN) have been sought as carriers for therapeutic proteins transport to the lung epithelium. Nevertheless, because of their low inertia, nanoparticles intended for pulmonary application usually escap...
Source: International Journal of Pharmaceutics - November 21, 2016 Category: Drugs & Pharmacology Source Type: research

Lipid vesicular nanocarrier: Quick encapsulation efficiency determination and transcutaneous application
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Yibang Zhang, Weibeng Ng, Xue Feng, Fangying Cao, Huaxi Xu Nanoscale delivery systems have been widely investigated to overcome the penetration barrier of stratum corneum for effective transcutaneous application. The aim of this study is the development of effective vesicular formulations of ovalbumin and saponin which are able to promote penetration through the skin layers. Three kinds of vesicular formulations have been investigated as carriers, including liposomes, transfersomes and ethosomes, in whi...
Source: International Journal of Pharmaceutics - November 21, 2016 Category: Drugs & Pharmacology Source Type: research

Polymeric nanospheres for topical delivery of vitamin D3
This study investigates the potential application of polymeric nanospheres (known as TyroSpheres) as a formulation carrier for topical delivery of cholecalciferol (i.e., Vitamin D3, VD3) with the goal to improve the skin delivery and stability of VD3. High drug loading and binding efficiencies were obtained for VD3 when loaded in TyroSpheres. VD3 was released from TyroSpheres in a sustained manner and was delivered across the stratum corneum, which occurred independent of the initial drug loading. An ex vivo skin distribution study showed that TyroSphere formulations delivered 3–10μg of active into the epidermis w...
Source: International Journal of Pharmaceutics - November 19, 2016 Category: Drugs & Pharmacology Source Type: research

Co-delivery of zinc and 5-aminosalicylic acid from alginate/N-succinyl-chitosan blend microspheres for synergistic therapy of colitis
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Haogang Duan, Shaoyu Lü, Hongyan Qin, Chunmei Gao, Xiao Bai, Yuhui Wei, Xin’an Wu, Mingzhu Liu, Xinyu Zhang, Zhen Liu The present study developed novel zinc ion cross-linked alginate/N-succinyl-chitosan (NSC) blend microspheres (MS) for co-delivery of zinc and 5-aminosalicylic acid (5-ASA) for synergistic therapy of colitis. Physicochemical characterization of blend MS was assessed using scanning electron microscopy (SEM), Fourier transform infrared (FTIR) spectroscopy, and energy dispersive ...
Source: International Journal of Pharmaceutics - November 19, 2016 Category: Drugs & Pharmacology Source Type: research

The effect of pulse duration, power and energy of fractional Er:YAG laser for transdermal delivery of differently sized FITC dextrans
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Barbara Zorec, Dejan Škrabelj, Marko Marinček, Damijan Miklavčič, Nataša Pavšelj We studied fractional Er:YAG laser to enhance transdermal drug delivery of compounds possessing different molecular weights: FITC-dextrans (or FD) with average molecular weights of 4, 10 and 20kDa. Vertical glass Franz diffusion cells were used to study molecular transport through dermatomed porcine skin and histological analysis of laser-treated skin was performed after treatment with different lase...
Source: International Journal of Pharmaceutics - November 19, 2016 Category: Drugs & Pharmacology Source Type: research

Development of hydroxyapatite nanoparticles loaded with folic acid to induce osteoblastic differentiation
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Catarina Santos, Pedro Gomes, José A. Duarte, Margarida M. Almeida, Maria E.V. Costa, Maria H. Fernandes Recently it has been shown that folic acid can have an important role in bone regeneration. For this reason, combining a classic bone regeneration system as, hydroxyapatite, loaded with folic acid, may be an important issue to be developed. To address this issue, hydroxyapatite nanoparticles loaded with folic acid were designed as an effective bone regenerative system, to induce osteoblast dif...
Source: International Journal of Pharmaceutics - November 18, 2016 Category: Drugs & Pharmacology Source Type: research

Microbial biosensors to monitor the encapsulation effectiveness of Doxorubicin in chimeric advanced Drug Delivery Nano Systems: A calorimetric approach
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Konstantinos Gardikis, Marco Signorelli, Chiara Ferrario, Alberto Schiraldi, Maria Grazia Fortina, Sophia Hatziantoniou, Costas Demetzos, Dimitrios Fessas The release of the anticancer drug doxorubicin (DOX) incorporated in a new drug carrier, namely a chimeric nanosystem formed by liposomes and dendrimers, was studied following the influence of the drug on the growth kinetics of the Lactobacillus helveticus bacterium, that would mimic the intestinal microflora. The bacterial growth was followed at 37&d...
Source: International Journal of Pharmaceutics - November 18, 2016 Category: Drugs & Pharmacology Source Type: research

Spray freeze drying as an alternative technique for lyophilization of polymeric and lipid-based nanoparticles
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Mohamed Ehab Ali, Alf Lamprecht The use of nanoparticles for drug delivery is still restricted by their limited stability when stored in an aqueous medium. Freeze drying is the standard method for long-term storage of colloidal nanoparticles; however the method needs to be elaborated for each formulation. Spray freeze drying (SFD) is proposed here as a promising alternative for lyophilizing colloidal nanoparticles. Different types of polymeric and lipid nanoparticles were prepared and characterized. Aft...
Source: International Journal of Pharmaceutics - November 18, 2016 Category: Drugs & Pharmacology Source Type: research

Biocompatibility and drug release behavior of curcumin conjugated gold nanoparticles from aminosilane-functionalized electrospun poly(N-vinyl-2-pyrrolidone) fibers
In this study, the 3-aminopropyltriethoxysilane (APTES)-functionalized electrospun poly(N-vinyl-2-pyrrolidone) fibers (NH2-PVP) were utilized as a free-standing substrate for the immobilization of CUR-PVP capped gold nanoparticles (CUR-PGNPs) conjugates. The conjugate was synthesized by sonication and the drug entrapment percentage was determined to be 54.2 ±1.8. CUR-PGNPs immobilized on NH2-PVP fibers showed a moderate burst release during the first few hours, followed by a sustained release lasting for 2days. The drug release was found pH-dependent (pH 5.0>6.0>7.4). The two-stage release profi...
Source: International Journal of Pharmaceutics - November 17, 2016 Category: Drugs & Pharmacology Source Type: research

Thermodynamics of aggregate formation between a non-ionic polymer and ionic surfactants: An isothermal titration calorimetric study
This report examines the energetics of aggregate formation between hydroxypropyl methylcellulose (HPMC) and model ionic surfactants including sodium dodecyl sulfate (SDS) at pharmaceutically relevant concentrations using the isothermal titration calorimetry (ITC) technique and a novel treatment of calorimetric data that accounts for the various species formed. The influence of molecular weight of HPMC, temperature and ionic strength of solution on the aggregate formation process was explored. The interaction between SDS and HPMC was determined to be an endothermic process and initiated at a critical aggregation concentrati...
Source: International Journal of Pharmaceutics - November 17, 2016 Category: Drugs & Pharmacology Source Type: research

The strategic relevance of manufacturing technology: An overall quality concept to promote innovation preventing drug shortage
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Michele Panzitta, Mauro Ponti, Giorgio Bruno, Giancarlo Cois, Alessandro D’Arpino, Paola Minghetti, Francesca Romana Mendicino, Luana Perioli, Maurizio Ricci Manufacturing is the bridge between research and patient: without product, there is no clinical outcome. Shortage has a variety of causes, in this paper we analyse only causes related to manufacturing technology and we use shortage as a paradigm highliting the relevance of Pharmaceutical Technology. Product and process complexity and capacity...
Source: International Journal of Pharmaceutics - November 17, 2016 Category: Drugs & Pharmacology Source Type: research

New nano-matrix oral formulation of nanoprecipitated cyclosporine A prepared with multi-inlet vortex mixer
We present a combined nanoparticle (NP) formation process and spray drying to create a nano-matrix formulation of cyclosporine A (CsA) and mannitol (nCsA/MAN) to increase the bioavailability of CsA. CsA NPs were prepared by flash nano precipitation (FNP) using a multi-inlet vortex mixer, and spray-dried with or without mannitol to prepare nCsA/MAN or nanoprecipitated CsA powder (nCsA), respectively. Pre-forming the NPs by FNP uncouples the sizes of the CsA inclusions from the ultimate micron-sized powders produced by spray drying. Both CsA formulations were physicochemically characterized, and a pharmacokinetic study in ra...
Source: International Journal of Pharmaceutics - November 16, 2016 Category: Drugs & Pharmacology Source Type: research

In-situ single pass intestinal permeability and pharmacokinetic study of developed Lumefantrine loaded solid lipid nanoparticles
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Anuj Garg, Kripal Bhalala, Devendra Singh Tomar, Wahajuddin The present investigation aims to develop lumefantrine loaded binary solid lipid nanoparticles (LF-SLNs) to improve its poor and variable oral bioavailability. The oral bioavailability of LF is poor and variable due to its limited aqueous solubility and P-gp mediated efflux occurring in small intestine. LF-SLNs were prepared using binary lipid mixture of stearic acid and caprylic acid stabilized with TPGS (D-alpha tocopheryl polyethylene glycol...
Source: International Journal of Pharmaceutics - November 16, 2016 Category: Drugs & Pharmacology Source Type: research

Polysaccharide-coated liposomal formulations for dental targeting
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Sara Pistone, Morten Rykke, Gro Smistad, Marianne Hiorth The efficacy of treatments of oral ailments is often challenged by a low residence time of the conventional pharmaceutical formulations in the oral cavity, which could be improved by using bioadhesive formulations. This in vitro study investigated charged liposomes, both uncoated and coated through electrostatic deposition with polysaccharides (chitosan, alginate and pectin), as bioadhesive systems for the oral cavity. First, formulations that pro...
Source: International Journal of Pharmaceutics - November 16, 2016 Category: Drugs & Pharmacology Source Type: research

Microfluidics platform for glass capillaries and its application in droplet and nanoparticle fabrication
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Bárbara Herranz-Blanco, Eloy Ginestar, Hongbo Zhang, Jouni Hirvonen, Hélder A. Santos The accessibility to microfluidics of a broader scientific community is often limited by the costly and complex manufacture of the chips. In this respect, we present a simple and reusable platform for the flexible and easy assembly of glass capillaries to create a microfluidics chip within minutes, with excellent chemical compatibility and durability, and without the need of using specialized infrastructu...
Source: International Journal of Pharmaceutics - November 16, 2016 Category: Drugs & Pharmacology Source Type: research

Impact of additives on the formation of protein aggregates and viscosity in concentrated protein solutions
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Katharina Christin Bauer, Susanna Suhm, Anna Katharina Wöll, Jürgen Hubbuch In concentrated protein solutions attractive protein interactions may not only cause the formation of undesired aggregates but also of gel-like networks with elevated viscosity. To guarantee stable biopharmaceutical processes and safe formulations, both phenomenons have to be avoided as these may hinder regular processing steps. This work screens the impact of additives on both phase behavior and viscosity of concentra...
Source: International Journal of Pharmaceutics - November 16, 2016 Category: Drugs & Pharmacology Source Type: research

Microfluidic manufacturing of phospholipid nanoparticles: Stability, encapsulation efficacy, and drug release
In this study, the microfluidic method for liposomes preparation is presented. DMPC and DSPC liposomes containing two different lipid/cholesterol ratios (1:1 and 2:1) are prepared. Results from this preparation process were compared with the film hydration method in order to understand benefits and drawbacks of microfluidics. Liposomes characterisation was evaluated through stability studies, encapsulation efficacy and drug release profiles of hydrophilic and lipophilic compounds. Stability tests were performed during 3 weeks and the liposomes properties of the most stable formulations were determined using Infrared Micros...
Source: International Journal of Pharmaceutics - November 15, 2016 Category: Drugs & Pharmacology Source Type: research

Improved formulation of cationic solid lipid nanoparticles displays cellular uptake and biological activity of nucleic acids
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Anna Fàbregas, Silvia Prieto, Marc Suñé-Pou, Sofía Boyero-Corral, Josep Ramón Ticó, Encarna García-Montoya, Pilar Pérez-Lozano, Montserrat Miñarro, Josep Mª Suñé-Negre, Cristina Hernández-Munain, Carlos Suñé Non-viral delivery using cationic solid lipid nanoparticles (SLNs) represents a useful strategy to introduce large DNA and RNA molecules to target cells. A careful selection of components and their...
Source: International Journal of Pharmaceutics - November 15, 2016 Category: Drugs & Pharmacology Source Type: research

Formulation and comparative in vitro evaluation of various dexamethasone-loaded pH-sensitive polymeric nanoparticles intended for dermal applications
In conclusion, various pH-sensitive nanoparticles that could release differently on the skin surface and dissolve and release in the hair follicles were obtained. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - November 15, 2016 Category: Drugs & Pharmacology Source Type: research

Folic acid-decorated and PEGylated PLGA nanoparticles for improving the antitumour activity of 5-fluorouracil
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Mazen M. El-Hammadi, Ángel V. Delgado, Consolación Melguizo, José C. Prados, José L. Arias 5-Fluorouracil (5-FU) is a broad spectrum cytotoxic agent being used in chemotherapy of malignancies. However, 5-FU shows a number of limitations like short half-life, non-selective biodistribution, and the development of drug resistances by tumour cells. It was investigated the potential use of folic acid-decorated and PEGylated poly(D,L-lactide-co-glycolide) nanoparticles (FOL-PEG-PLG...
Source: International Journal of Pharmaceutics - November 15, 2016 Category: Drugs & Pharmacology Source Type: research

The effects of hydration media on the characteristics of non-ionic surfactant vesicles (NISV) prepared by microfluidics
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Mohammad A. Obeid, Ibrahim Khadra, Alexander B. Mullen, Rothwelle J. Tate, Valerie A. Ferro Non-ionic surfactant vesicles (NISV) are colloidal particles that provide a useful delivery system for drugs and vaccines. One of the methods that is used for NISV preparation is microfluidics in which the lipid components dissolved in organic phase are mixed with an aqueous medium to prepare the particles through self-assembly of the lipids. In this work, we examined the effect of using different types of aqueou...
Source: International Journal of Pharmaceutics - November 15, 2016 Category: Drugs & Pharmacology Source Type: research

Ionic liquids as potential enhancers for transdermal drug delivery
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Daniela Monti, Emanuele Egiziano, Susi Burgalassi, Patrizia Chetoni, Cinzia Chiappe, Angelo Sanzone, Silvia Tampucci The aim of this study was to verify the effect of several cyclic onium based ionic liquids (ILs), including mono- and dicationic derivatives of 1,4-diazabicyclo[2.2.2]octane (DABCO), a dialkyl morpholinium salt and a Brønsted acidic IL, as enhancers of the in vitro transdermal permeation and skin retention of diltiazem through and into hairless rat skin. The drug was used as both t...
Source: International Journal of Pharmaceutics - November 15, 2016 Category: Drugs & Pharmacology Source Type: research

Development of near zero-order release PLGA-based microspheres of a novel antipsychotic
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Jinlong Zhao, Lexi Wang, Chunyu Fan, Kongtong Yu, Ximing Liu, Xiaolei Zhao, Dan Wang, Wenhua Liu, Zhengxing Su, Fengying Sun, Youxin Li The novel antipsychotic isoperidone, a prodrug of paliperidone, was designed to improve liposolubility for the development of poly(D,L-lactide-co-glycolide) (PLGA)-based microspheres to achieve near zero-order release behaviour in vivo. Microspheres with a smooth surface were obtained using the oil-in-water emulsion solvent evaporation method and yielded a high encapsul...
Source: International Journal of Pharmaceutics - November 15, 2016 Category: Drugs & Pharmacology Source Type: research

The effect of material attributes and process parameters on the powder bed uniformity during a low-dose dosator capsule filling process
The objective of this work was to assess the effect of process parameters of a dosator nozzle machine on the powder bed uniformity of inhalation powders with various characteristics during a low-dose dosator capsule filling process. Three grades of lactose excipients were extensively characterized and filled into size 3 capsules using different dosing chamber lengths (2.5, 5mm), nozzle diameters (1.9, 3.4mm), powder bed heights (5, 10mm) and filling speeds (500, 3000capsules/h). The fill weight and the weight variability of Lactohale 100 (large particles, good flowability, low cohesion) remained almost the same, regardless...
Source: International Journal of Pharmaceutics - November 15, 2016 Category: Drugs & Pharmacology Source Type: research

Polymeric particle-mediated molecular therapies to treat spinal cord injury
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Farideh Ordikhani, Saahil Sheth, Silviya Petrova Zustiak Spinal cord injury (SCI) is a physically and psychologically debilitating condition that mainly affects young, healthy males who are at the peak of their personal and professional development. SCI damages axons and disrupts myelination, which interrupts sensory and motor neuronal function. Current treatments are mostly palliative, aimed at reducing further damage and pain, but do not provide a cure. Polymeric particles have shown tremendous promis...
Source: International Journal of Pharmaceutics - November 15, 2016 Category: Drugs & Pharmacology Source Type: research

Poly vinyl acetate and ammonio methacrylate copolymer as unconventional polymer blends increase the mechanical robustness of HPMC matrix tablets
Conclusion Poly vinyl acetate and ammonio methacrylate copolymer could be a proper polymer blend for coating HPMC matrix tablets to increase mechanical robustness, which characterized by its flexibility and permeability. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - November 14, 2016 Category: Drugs & Pharmacology Source Type: research

Osmolality of antisense oligonucleotide parenteral formulations: Implications on counterion dissociation and recommended osmometry techniques
Publication date: 30 December 2016 Source:International Journal of Pharmaceutics, Volume 515, Issues 1–2 Author(s): Marc Lim, Andrew Dibble The intrinsic osmolality of aqueous solutions of sodium salt antisense oligonucleotides (ASOs) has been studied to inform formulation practices, understand the molecular basis underlying the difference between theoretical and empirical results, and determine suitable measurement methods. It was found that regardless of nucleotide sequence, ASO concentration of ∼140mg/mL has isotonic osmolality of ∼290mOsm/kg water (SI unit: mmol osmotically-active particles/kg water), su...
Source: International Journal of Pharmaceutics - November 12, 2016 Category: Drugs & Pharmacology Source Type: research

Evaluation of Pentravan ®, Pentravan® Plus, Phytobase®, Lipovan® and Pluronic Lecithin Organogel for the transdermal administration of antiemetic drugs to treat chemotherapy-induced nausea and vomiting at the hospital
The objective of this study was to evaluate five commercial ready-to-use transdermal vehicles (Phytobase®, Lipovan®, Pentravan®, Pentravan® Plus and Pluronic Lecithin Organogel (PLO)), for the compounding of three antiemetic drugs (ondansetron, dexamethasone and aprepitant) and their administration in combination to treat chemotherapy-induced nausea and vomiting (CINV) at the hospital. Drugs were individually formulated in these vehicles and in mixture in Pentravan® Plus using different penetration enhancers. Quality control of the forms has demonstrated that formulation process was mastered and conveni...
Source: International Journal of Pharmaceutics - November 12, 2016 Category: Drugs & Pharmacology Source Type: research

Style and precision in scientific papers
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Alexander T. Florence (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - November 12, 2016 Category: Drugs & Pharmacology Source Type: research

Efficient approach to enhance drug solubility by particle engineering of bovine serum albumin
Publication date: 30 December 2016 Source:International Journal of Pharmaceutics, Volume 515, Issues 1–2 Author(s): Mouhamad Khoder, Hamdy Abdelkader, Amr ElShaer, Ayman Karam, Mohammad Najlah, Raid G. Alany The aim of this study was to investigate the use of bovine serum albumin (BSA) as a solubility enhancer for indometacin (IND) as a model drug. IND-BSA solid dispersions were prepared by both spray drying and freeze drying techniques using IND:BSA solution (20:1 Molar Ratio (MR)) and IND:BSA suspension (100:1 MR). The solid state of IND in solid dispersions was characterised by SEM, DSC and XRD. The aqueous solub...
Source: International Journal of Pharmaceutics - November 10, 2016 Category: Drugs & Pharmacology Source Type: research

Where does hydrolysis of nandrolone decanoate occur in the human body after release from an oil depot?
Publication date: 30 December 2016 Source:International Journal of Pharmaceutics, Volume 515, Issues 1–2 Author(s): R.W. Kalicharan, M.R. Bout, C. Oussoren, H. Vromans Long-term therapy of nandrolone (N) is recommended to increase mineral density and muscle strength. Using a parenteral sustained release drug formulation with nandrolone decanoate (ND), therapeutic N levels can be achieved and maintained. Until now, it is unknown if hydrolysis of ND into N occurs in tissue at the injection site or after systemic absorption. Therefore, hydrolysis studies were conducted to investigate the location and rate of ND hydroly...
Source: International Journal of Pharmaceutics - November 10, 2016 Category: Drugs & Pharmacology Source Type: research

Impact of sodium chloride on the expansion of a liquid-liquid miscibility gap in an API/water system. Case study of Brivaracetam
Publication date: 30 December 2016 Source:International Journal of Pharmaceutics, Volume 515, Issues 1–2 Author(s): Nicolas Couvrat, Julien Mahieux, Baptiste Fours, Yohann Cartigny, Eric Schenkel, Luc Aerts, Luc Quéré, Gérard Coquerel Brivaracetam, or (2S)-2-[(4R)-2-oxo-4-propyl-pyrrolidin-1-yl] butanamide, is an active pharmaceutical ingredient designed for the treatment of epilepsy. During the development of the IV administration mode, a liquid-liquid miscibility gap has been observed with pure water, isotonic and hypertonic solutions (vehicle at 0.9% w/w and 5%w/w NaCl respectively). The stud...
Source: International Journal of Pharmaceutics - November 10, 2016 Category: Drugs & Pharmacology Source Type: research

Encapsulation of NSAIDs for inflammation management: Overview, progress, challenges and prospects
Publication date: 30 December 2016 Source:International Journal of Pharmaceutics, Volume 515, Issues 1–2 Author(s): Waisudin Badri, Karim Miladi, Qand Agha Nazari, Hélène Greige-Gerges, Hatem Fessi, Abdelhamid Elaissari Non-steroidal anti-inflammatory drugs (NSAIDs) are among the most widely prescribed drugs. Debilitating diseases such as rheumatoid arthritis and osteoarthritis are commonly managed by NSAIDs. However, NSAIDs pharmacological mechanism is often associated with the presence of gastrointestinal side effects. NSAIDs encapsulation is performed in order to overcome some of the drawbacks linke...
Source: International Journal of Pharmaceutics - November 10, 2016 Category: Drugs & Pharmacology Source Type: research

Oral sustained-release suspension based on a lauryl sulfate salt/complex
The objective of this study was to evaluate the feasibility of lauryl sulfate (LS) salt/complex as a novel carrier in oral sustained-release suspensions. Mirabegron, which has a pH-dependent solubility, was selected as the model drug. Sodium lauryl sulfate (SLS) was bound to mirabegron in a stoichiometric manner to form an LS salt/complex. LS salt/complex formulation significantly reduced the solubility of mirabegron and helped mirabegron achieve sustained-release over a wide range of pH conditions. Microparticles containing the LS salt/complex were prepared by spray drying with the aqueous dispersion of ethylcellulose (Aq...
Source: International Journal of Pharmaceutics - November 8, 2016 Category: Drugs & Pharmacology Source Type: research

Complexation of curcumin with 2-aminoethyl diphenyl borate and implications for spatiotemporal fluorescence monitoring
In this study, we successfully determined spatiotemporal distribution of curcumin in mice via simple and fast fluorescence detection of native curcumin and stabilized curcumin. We used 2-aminoethyl diphenyl borate (DPBA) as a stabilizer of curcumin, which binds to curcumin and enhances its aqueous stability. After intravenous injection, curcumin and DPBA–curcumin complexes showed similar fluorescence intensities in the brain, pancreas, lungs, and kidneys at 15min. However, stabilized DPBA–curcumin complexes exhibited much stronger fluorescent signals at metabolically active sites such as liver tissues than nati...
Source: International Journal of Pharmaceutics - November 8, 2016 Category: Drugs & Pharmacology Source Type: research

Rapid and cost-effective xenograft hepatocellular carcinoma model in Zebrafish for drug testing
In conclusion, the possibility to test anti HCC/neo-angiogenesis drugs makes our JHH6 model useful to select therapeutic molecules for a highly vascularized tumor such as HCC. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - November 3, 2016 Category: Drugs & Pharmacology Source Type: research