A preliminary study for the development and optimization by experimental design of an in vitro method for prediction of drug buccal absorption
Publication date: 25 August 2018 Source:International Journal of Pharmaceutics, Volume 547, Issues 1–2 Author(s): Paola Mura, Serena Orlandini, Marzia Cirri, Francesca Maestrelli, Natascia Mennini, Giada Casella, Sandra Furlanetto The work was aimed at developing an in vitro method able to provide rapid and reliable evaluation of drug absorption through buccal mucosa. Absorption simulator apparatus endowed with an artificial membrane was purposely developed by experimental design. The apparent permeation coefficient (Papp) through excised porcine buccal mucosa of naproxen, selected as model drug, was the target valu...
Source: International Journal of Pharmaceutics - June 16, 2018 Category: Drugs & Pharmacology Source Type: research

Multivariate monitoring for the industrialisation of a continuous wet granulation tableting process
Publication date: 25 August 2018 Source:International Journal of Pharmaceutics, Volume 547, Issues 1–2 Author(s): Simeone Zomer, Jun Zhang, Sameer Talwar, Sayantan Chattoraj, Christopher Hewitt The pharmaceutical industry is undergoing a significant change in product development and manufacturing strategies with the progressive shift from batch to continuous processes. These typically feature vast volumes of data generated by the numerous sensors connected to several unit operations running over the period of several hours or even days and that demand the application of increasingly efficient tools for process under...
Source: International Journal of Pharmaceutics - June 16, 2018 Category: Drugs & Pharmacology Source Type: research

Chitosan based polymer-lipid hybrid nanoparticles for oral delivery of enoxaparin
In conclusion, GMO/CS based PLNs can provide a new insight to develop orally applicable delivery system for hydrophilic macromolecules. Their absorption can be enhanced with proposed PLNs and preparation of this PLNs was also found to be easy comparing to other similar methods. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - June 16, 2018 Category: Drugs & Pharmacology Source Type: research

Formulation techniques for high dose dry powders
Publication date: 25 August 2018 Source:International Journal of Pharmaceutics, Volume 547, Issues 1–2 Author(s): Ashlee D. Brunaugh, Hugh D.C. Smyth Delivery of drugs to the lungs via dry powder inhaler (DPI) is a promising approach for the treatment of both local pulmonary conditions and systemic diseases. Though DPIs are widely used for the pulmonary deposition of potent bronchodilators, anticholinergics, and corticosteroids, there is growing interest in the utilization of this delivery system for the administration of high drug doses to the lungs, as made evident by recent regulatory approvals for anti-microbial...
Source: International Journal of Pharmaceutics - June 15, 2018 Category: Drugs & Pharmacology Source Type: research

Visual validation of the measurement of entrapment efficiency of drug nanocarriers
In conclusion, the ultrafiltration method is the method of choice for efficient separation and accurate measurement of EE. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - June 15, 2018 Category: Drugs & Pharmacology Source Type: research

A new therapeutic avenue for bronchiectasis: Dry powder inhaler of ciprofloxacin nanoplex exhibits superior ex vivo mucus permeability and antibacterial efficacy to its native ciprofloxacin counterpart
Publication date: 25 August 2018 Source:International Journal of Pharmaceutics, Volume 547, Issues 1–2 Author(s): The-Thien Tran, Celine Vidaillac, Hong Yu, Valerie F.L. Yong, Dan Roizman, Ravishankar Chandrasekaran, Albert Y.H. Lim, Teck Boon Low, Gan Liang Tan, John A. Abisheganaden, Mariko Siyue Koh, Jeanette Teo, Sanjay H. Chotirmall, Kunn Hadinoto Non-cystic fibrosis bronchiectasis (NCFB) characterized by permanent bronchial dilatation and recurrent infections has been clinically managed by long-term intermittent inhaled antibiotic therapy among other treatments. Herein we investigated dry powder inhaler (DPI) ...
Source: International Journal of Pharmaceutics - June 15, 2018 Category: Drugs & Pharmacology Source Type: research

Development of fluorometholone-loaded PLGA nanoparticles for treatment of inflammatory disorders of anterior and posterior segments of the eye
Publication date: 25 August 2018 Source:International Journal of Pharmaceutics, Volume 547, Issues 1–2 Author(s): Roberto Gonzalez-Pizarro, Marcelle Silva-Abreu, Ana Cristina Calpena, María Antonia Egea, Marta Espina, María Luisa García The main objective of this study was the development and optimization of fluorometholone-loaded PLGA nanoparticles for the treatment of inflammatory conditions of the eye. Design of experiments was used to obtain nanoparticles with the best physicochemical characteristics. The optimized nanoparticles containing 1.5 mg·mL−1 of fluorometholone showed...
Source: International Journal of Pharmaceutics - June 15, 2018 Category: Drugs & Pharmacology Source Type: research

Development of self-emulsifying drug delivery systems (SEDDS) for ciprofloxacin with improved mucus permeating properties
Publication date: 25 August 2018 Source:International Journal of Pharmaceutics, Volume 547, Issues 1–2 Author(s): Sergey Zaichik, Christian Steinbring, Claudia Menzel, Ludwig Knabl, Dorothea Orth-Höller, Helmut Ellemunter, Katharina Niedermayr, Andreas Bernkop-Schnürch The aim of this study was to develop a self-emulsifying drug delivery system (SEDDS) containing the fluoroquinolone antibiotic ciprofloxacin (CIP) exhibiting highly mucus permeating properties and antimicrobial activity in in vitro models. Various SEDDS formulations were developed and evaluated regarding droplet size, polydispersity index, z...
Source: International Journal of Pharmaceutics - June 15, 2018 Category: Drugs & Pharmacology Source Type: research

Strat-M ® synthetic membrane: Permeability comparison to human cadaver skin
Publication date: 25 August 2018 Source:International Journal of Pharmaceutics, Volume 547, Issues 1–2 Author(s): Anika Haq, Benjamin Goodyear, Dina Ameen, Vivek Joshi, Bozena Michniak-Kohn The aim of this work was to investigate the correlation of permeation behavior of transdermal formulations through a novel synthetic membrane (Strat-M® EMD Millipore, MA) and human cadaver skin. Strat-M® membranes were designed with the intent to share similar structural and chemical characteristics found in the human skin however, omitting any biological behavior due to the absence of viable cells. Both human skin and th...
Source: International Journal of Pharmaceutics - June 15, 2018 Category: Drugs & Pharmacology Source Type: research

Real-time feedback control of twin-screw wet granulation based on image analysis
Publication date: 25 August 2018 Source:International Journal of Pharmaceutics, Volume 547, Issues 1–2 Author(s): Lajos Madarász, Zsombor Kristóf Nagy, István Hoffer, Barnabás Szabó, István Csontos, Hajnalka Pataki, Balázs Démuth, Bence Szabó, Kristóf Csorba, György Marosi The present paper reports the first dynamic image analysis-based feedback control of continuous twin-screw wet granulation process. Granulation of the blend of lactose and starch was selected as a model process. The size and size distribution of the obtained particles were ...
Source: International Journal of Pharmaceutics - June 15, 2018 Category: Drugs & Pharmacology Source Type: research

Isoniazid-loaded orodispersible strips: Methodical design, optimization and in vitro-in silico characterization
Publication date: 25 August 2018 Source:International Journal of Pharmaceutics, Volume 547, Issues 1–2 Author(s): Oluwatoyin A. Adeleke, Pei-Chin Tsai, Krizia M. Karry, Nkwe O. Monama, Bozena B. Michniak-Kohn Drug treatment remains the most effective global approach to managing and preventing tuberculosis. This work focuses on formulating and evaluating an optimized polyvinyl alcohol-polyethylene glycol based orodispersible strip containing isoniazid, a first-line anti-tubercular agent. A solvent casting method guided through a Taguchi experimental design was employed in the fabrication, optimization and characteriz...
Source: International Journal of Pharmaceutics - June 15, 2018 Category: Drugs & Pharmacology Source Type: research

Laser based thermo-conductometry as an approach to determine ribbon solid fraction off-line and in-line
This study showed the potentials of this new technique and is a starting point for additional work that has to be done to overcome these challenges. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - June 15, 2018 Category: Drugs & Pharmacology Source Type: research

Targeted delivery of pixantrone to neutrophils by poly(sialic acid)-p-octadecylamine conjugate modified liposomes with improved antitumor activity
Publication date: 25 August 2018 Source:International Journal of Pharmaceutics, Volume 547, Issues 1–2 Author(s): Xiang Luo, Mingqi Liu, Ling Hu, Qiujun Qiu, Xinrong Liu, Cong Li, Mei Lu, Yang Liu, Ting Zhang, Songlei Zhou, David Julian McClements, Xian Jia, Yihui Deng, Yanzhi Song Based on the knowledge that poly(sialic acid) is a critical element for tumour development and that the receptors for its monomer are expressed on neutrophils, which play important roles in the progression and invasion of tumours, a poly(sialic acid)-p-octadecylamine conjugate (PSA-p-ODA) was synthesised and used to modify the surface of ...
Source: International Journal of Pharmaceutics - June 15, 2018 Category: Drugs & Pharmacology Source Type: research

Self-assembled liposome from multi-layered fibrous mucoadhesive membrane for buccal delivery of drugs having high first-pass metabolism
Publication date: 25 August 2018 Source:International Journal of Pharmaceutics, Volume 547, Issues 1–2 Author(s): Jianting Chen, Hao Pan, Yining Yang, Shihang Xiong, Hongliang Duan, Xinggang Yang, Weisan Pan A novel delivery system based on self-assembled liposome from multi-layered fibrous mucoadhesive membrane has been developed to improve the bioavailability of Carvedilol (Car). This system consisted of an electrospun layer (enable self-assembly of liposome once contacting with water), an adhesive layer (prolong the retention period in the mouth) and a backing layer. SEM, DSC and FTIR were applied to characterize...
Source: International Journal of Pharmaceutics - June 15, 2018 Category: Drugs & Pharmacology Source Type: research

Effect of delayed pMDI actuation on the lung deposition of a fixed-dose combination aerosol drug
Publication date: 25 August 2018 Source:International Journal of Pharmaceutics, Volume 547, Issues 1–2 Author(s): Árpád Farkas, Alpár Horváth, Attila Kerekes, Attila Nagy, Szilvia Kugler, Lilla Tamási, Gábor Tomisa Lack of coordination between the beginning of the inhalation and device triggering is one of the most frequent errors reported in connection with the use of pMDI devices. Earlier results suggested a significant loss in lung deposition as a consequence of late actuation. However, most of our knowledge on the effect of poor synchronization is based on earlier works ...
Source: International Journal of Pharmaceutics - June 15, 2018 Category: Drugs & Pharmacology Source Type: research

RTD-based material tracking in a fully-continuous dry granulation tableting line
Publication date: 25 August 2018 Source:International Journal of Pharmaceutics, Volume 547, Issues 1–2 Author(s): M.C. Martinetz, A-P. Karttunen, S. Sacher, P. Wahl, J. Ketolainen, J.G. Khinast, O. Korhonen Continuous manufacturing (CM) offers quality and cost-effectiveness benefits over currently dominating batch processing. One challenge that needs to be addressed when implementing CM is traceability of materials through the process, which is needed for the batch/lot definition and control strategy. In this work the residence time distributions (RTD) of single unit operations (blender, roller compactor and tablet ...
Source: International Journal of Pharmaceutics - June 15, 2018 Category: Drugs & Pharmacology Source Type: research

Promising nanotherapy in treating leishmaniasis
Publication date: 25 August 2018 Source:International Journal of Pharmaceutics, Volume 547, Issues 1–2 Author(s): Aline de Souza, Débora Soares Souza Marins, Samir Leite Mathias, Lis Marie Monteiro, Megumi Nishitani Yukuyama, Cauê Benito Scarim, Raimar Löbenberg, Nádia Araci Bou-Chacra Leishmaniases are infectious diseases caused by an intracellular protozoan in humans by 20 different species of Leishmania among more than 53 species. There are at least twelve million cases of infections worldwide and three hundred and fifty million people are at risk in at least 98 developing countries in Af...
Source: International Journal of Pharmaceutics - June 15, 2018 Category: Drugs & Pharmacology Source Type: research

Pharmaceutical cocrystallization techniques. Advances and challenges
Publication date: 25 August 2018 Source:International Journal of Pharmaceutics, Volume 547, Issues 1–2 Author(s): Marisa Rodrigues, Bárbara Baptista, João Almeida Lopes, Mafalda Cruz Sarraguça Cocrystals are homogenous (single-phase) crystalline structures composed by two or more components in a definite stoichiometric ratio bonded together by noncovalent bonds. Pharmaceutical industry has been showing interest in cocrystals due to their ability to improve active pharmaceutical ingredients (API’s) properties, such as solubility, dissolution, bioavailability, stability and processability. T...
Source: International Journal of Pharmaceutics - June 15, 2018 Category: Drugs & Pharmacology Source Type: research

Effect of photo-degradation on the structure, stability, aggregation, and function of an IgG1 monoclonal antibody
Publication date: 25 August 2018 Source:International Journal of Pharmaceutics, Volume 547, Issues 1–2 Author(s): Dinen D. Shah, Jingming Zhang, Haripada Maity, Krishna M.G. Mallela Photostability testing of therapeutic proteins is a critical requirement in the development of biologics. Upon exposure to light, pharmaceutical proteins may undergo a change in structure, stability, and functional properties that could have a potential impact on safety and efficacy. In this work, we studied how exposure to light, according to ICH guidelines, leads to photo-oxidation of a therapeutic IgG1 mAb. We also tested the ability ...
Source: International Journal of Pharmaceutics - June 14, 2018 Category: Drugs & Pharmacology Source Type: research

Chemical modifications of insulin: Finding a compromise between stability and pharmaceutical performance
Publication date: 25 August 2018 Source:International Journal of Pharmaceutics, Volume 547, Issues 1–2 Author(s): Mohsen Akbarian, Younes Ghasemi, Vladimir N. Uversky, Reza Yousefi Insulin, a key peptide hormone that conjointly with its receptor regulates blood glucose levels, is used as the major means to treat diabetes. This therapeutic hormone may undergo different chemical modifications during industrial processes, pharmaceutical formulation, and through its endogenous storage in the pancreatic β-cells. Insulin is highly sensitive to the environmental stresses and easily undergoes structural changes, being ...
Source: International Journal of Pharmaceutics - June 14, 2018 Category: Drugs & Pharmacology Source Type: research

pH-Responsive hyaluronated liposomes for docetaxel delivery
In this study, we report pH-responsive liposomes consisting of hydrogenated soy phosphatidylcholine (HSPC) as a lipid, hyaluronic acid (HA) grafted with functional 3-diethylaminopropyl (DEAP) groups (hereafter denoted as HA-g-DEAP) as a pH-responsive polymer, and docetaxel (DTX) as an antitumor drug. DTX-loaded HSPC liposomes were prepared via a conventional liposome manufacturing procedure and then were decorated with HA-g-DEAP (HA-g-DEAP0.15, HA-g-DEAP0.25, and HA-g-DEAP0.40, according to the molar conjugate ratio of DEAP to HA) in an aqueous solution (pH 7.4), by sonication. The liposomes with HA-g-DEAP0.40 allowed the ...
Source: International Journal of Pharmaceutics - June 12, 2018 Category: Drugs & Pharmacology Source Type: research

The use of low molecular weight protamine to enhance oral absorption of exenatide
In this study, we constructed a zinc ion (Zn2+) and exenatide complex functionalized nanoparticle (NP) oral delivery system to overcome the above-mentioned issue. Polyethylene glycol-poly(lactic-co-glycolic acid) (PEG-PLGA) was used as a drug carrier to escape enzymatic degradation in the gastrointestinal tract, and low molecular weight protamine (LMWP) was used as a functional group to increase penetration of NPs into the intestinal epithelium. The functionalized NPs exhibited significantly improved penetration across the intestinal epithelium, as shown by cell uptake and transmembrane transport experiments. Moreover, a s...
Source: International Journal of Pharmaceutics - June 8, 2018 Category: Drugs & Pharmacology Source Type: research

Calcium enhances gene expression when using low molecular weight poly-l-lysine delivery vehicles
Publication date: 25 August 2018 Source:International Journal of Pharmaceutics, Volume 547, Issues 1–2 Author(s): Sheng-Xue Xie, Abdulgader A. Baoum, Nabil A. Alhakamy, Cory J. Berkland Four molecular weights of poly-l-lysine (PLL) [1000–5000 Da, 1500–8000 Da, 4000–15,000 Da and 15,000–30,000 Da] and three molecular weights of polyethyleneimine (PEI) [800 Da, 2,000 Da, and 25,000 Da] were used to systematically study the effect of calcium (Ca2+) to improve transfection efficiency of polyelectrolyte complexes. Complexes made using different molecular weights of PLL or PEI polymer...
Source: International Journal of Pharmaceutics - June 8, 2018 Category: Drugs & Pharmacology Source Type: research

Phase transitions of antibiotic clarithromycin forms I, IV and new form VII crystals
Publication date: 25 August 2018 Source:International Journal of Pharmaceutics, Volume 547, Issues 1–2 Author(s): Masataka Ito, Rika Shiba, Miteki Watanabe, Yasunori Iwao, Shigeru Itai, Shuji Noguchi Metastable crystal form I of the antibiotic clarithromycin has a pharmaceutically valuable characteristic that its crystalline phase transition can be applied for its sustained release from tablets. The phase transition of form I was investigated in detail by single crystal and powder X-ray analyses, dynamic vapor sorption analysis and thermal analysis. The single crystal structure of form I revealed that form I was not...
Source: International Journal of Pharmaceutics - June 8, 2018 Category: Drugs & Pharmacology Source Type: research

Immunogenicity of diphtheria toxoid and poly(I:C) loaded cationic liposomes after hollow microneedle-mediated intradermal injection in mice
In this study, we aimed to investigate the immunogenicity of cationic liposomes loaded with diphtheria toxoid (DT) and poly(I:C) after hollow microneedle-mediated intradermal vaccination in mice. The following liposomal formulations were studied: DT loaded liposomes, a mixture of free DT and poly(I:C)-loaded liposomes, a mixture of DT-loaded liposomes and free poly(I:C), and liposomal formulations with DT and poly(I:C) either individually or co-encapsulated in the liposomes. Reference groups were DT solution adjuvanted with or without poly(I:C) (DT/poly(I:C)). The liposomal formulations were characterized in terms of parti...
Source: International Journal of Pharmaceutics - June 7, 2018 Category: Drugs & Pharmacology Source Type: research

Layer-by-layer nanocoating of antibacterial niosome on orthopedic implant
Publication date: 25 August 2018 Source:International Journal of Pharmaceutics, Volume 547, Issues 1–2 Author(s): Anupma Dwivedi, Anisha Mazumder, Norased Nasongkla The major clinical hindrance of orthopedic implants is the bacterial infection, which can lead to biofilm formation and ultimately results in implant rejection. In this research, layer-by-layer nanocoating consists of vancomycin/PLA/vancomycin-loaded niosomes was designed. Vancomycin-loaded niosomes were formulated by thin film hydration method and the attributes of niosomes in terms of size, zeta potential, drug loading and EE, were assessed. The size w...
Source: International Journal of Pharmaceutics - June 6, 2018 Category: Drugs & Pharmacology Source Type: research

Rapid paper based colorimetric detection of glucose using a hollow microneedle device
Publication date: 25 August 2018 Source:International Journal of Pharmaceutics, Volume 547, Issues 1–2 Author(s): Dean Nicholas, Keiran A. Logan, Yingjie Sheng, Jinhui Gao, Sian Farrell, Dorian Dixon, Bridgeen Callan, Anthony P. McHale, John F. Callan The monitoring of blood glucose is a key aspect of diabetes care in limiting the negative effects of hyperglycaemia to both the microvasculature and macrovasculature. Self-monitoring of blood glucose (SMBG) gives an indication of blood glucose at a specific point in time and is recommended to be carried out four times daily. However, due to the inconvenience and associ...
Source: International Journal of Pharmaceutics - June 6, 2018 Category: Drugs & Pharmacology Source Type: research

Effect of glycerol on the physical and mechanical properties of thin gellan gum films for oral drug delivery
Publication date: 25 August 2018 Source:International Journal of Pharmaceutics, Volume 547, Issues 1–2 Author(s): Patrizia Paolicelli, Stefania Petralito, Gabriele Varani, Martina Nardoni, Settimio Pacelli, Laura Di Muzio, Jacopo Tirillò, Cecilia Bartuli, Stefania Cesa, Maria Antonietta Casadei, Alessandra Adrover In this work, deacylated gellan gum and the plasticizer glycerol were used as primary components for the preparation of thin films intended for the oral delivery of therapeutic molecules. The samples were prepared by a solvent casting method and characterized for their thickness, tensile properties,...
Source: International Journal of Pharmaceutics - June 5, 2018 Category: Drugs & Pharmacology Source Type: research

Enhanced anti-tumor and anti-metastasis efficacy against breast cancer with an intratumoral injectable phospholipids-based phase separation gel co-loaded with 5-fluotouracil and magnesium oxide by neutralizing acidic microenvironment
In conclusion, the novel 5FU + MgO-PPSG system might have a great potential to improve treatment method against breast metastasis. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - June 3, 2018 Category: Drugs & Pharmacology Source Type: research

Nanostructured lipid carriers-based drug delivery for treating various lung diseases: A State ‐of‐the‐Art Review
Publication date: 25 August 2018 Source:International Journal of Pharmaceutics, Volume 547, Issues 1–2 Author(s): Tulshidas S. Patil, Ashwini S. Deshpande According to the list published by the WHO for global top ten causes of death, lung diseases contribute nearly one-third of the total mortality. The current treatment on lung diseases provide only symptomatic relief rather than restoring the complete lung functions. Nanostructured lipid carriers-based drug delivery system (NLCs-based DDS) provide a breakthrough in treating various lung diseases. This review provides the readers with background information for rati...
Source: International Journal of Pharmaceutics - June 3, 2018 Category: Drugs & Pharmacology Source Type: research

Surface-induced crystallization of pharmaceuticals and biopharmaceuticals: A review
Publication date: 25 August 2018 Source:International Journal of Pharmaceutics, Volume 547, Issues 1–2 Author(s): Fiora Artusio, Roberto Pisano Despite the wide occurrence of crystallization in the pharmaceutical industry, deep understanding and fine control of the process remain a tricky issue. Nevertheless, the successful manufacturing of finished pharmaceutical products, as well as the structural determination of biopharmaceuticals, depend on the size, form, shape and purity of the crystals. The ability of substrates with precise chemistry and topological features to induce nucleation has been thoroughly assessed...
Source: International Journal of Pharmaceutics - June 3, 2018 Category: Drugs & Pharmacology Source Type: research

Pharmaceutical-grade oral films as substrates for printed medicine
Publication date: 25 August 2018 Source:International Journal of Pharmaceutics, Volume 547, Issues 1–2 Author(s): M. Wimmer-Teubenbacher, C. Planchette, H. Pichler, D. Markl, W.K. Hsiao, A. Paudel, S. Stegemann In contact-less printing, such as piezo-electric drop on demand printing used in the study, the drop formation process is independent of the substrate. This means that having developed a printable formulation, printed pharmaceutical dosage forms can be obtained on any pharmaceutical grade substrate, such as polymer-based films. In this work we evaluated eight different oral films based on their suitability as...
Source: International Journal of Pharmaceutics - June 2, 2018 Category: Drugs & Pharmacology Source Type: research

Preparation and optimization of a dry powder for inhalation of second-line anti-tuberculosis drugs
Publication date: 25 August 2018 Source:International Journal of Pharmaceutics, Volume 547, Issues 1–2 Author(s): Rajeev Ranjan, Ashish Srivastava, Reena Bharti, Lipika Ray, Jyotsna Singh, Amit Misra A spray drying process was standardized to prepare an inhalable powder comprising d-cycloserine and ethionamide, two “second line” drugs employed for treating multi-drug resistant (MDR) tuberculosis (TB). The aim of the process development effort was to maximize product yield. Contour plots were generated using a small central composite design (CCD) with face centered (α = 1) to maximize the proces...
Source: International Journal of Pharmaceutics - June 2, 2018 Category: Drugs & Pharmacology Source Type: research

The effects of three absorption-modifying critical excipients on the in vivo intestinal absorption of six model compounds in rats and dogs
Publication date: 25 August 2018 Source:International Journal of Pharmaceutics, Volume 547, Issues 1–2 Author(s): D. Dahlgren, C. Roos, P. Johansson, C. Tannergren, A. Lundqvist, P. Langguth, M. Sjöblom, E. Sjögren, H. Lennernäs Pharmaceutical excipients that may affect gastrointestinal (GI) drug absorption are called critical pharmaceutical excipients, or absorption-modifying excipients (AMEs) if they act by altering the integrity of the intestinal epithelial cell membrane. Some of these excipients increase intestinal permeability, and subsequently the absorption and bioavailability of the drug. This...
Source: International Journal of Pharmaceutics - June 2, 2018 Category: Drugs & Pharmacology Source Type: research

Deformation behavior of crystallized mannitol during compression using a rotary tablet press simulator
Publication date: 25 August 2018 Source:International Journal of Pharmaceutics, Volume 547, Issues 1–2 Author(s): Nicolas Tarlier, Ian Soulairol, Noelia Sanchez-Ballester, Gilles Baylac, Adrien Aubert, Philippe Lefevre, Bernard Bataille, Tahmer Sharkawi Mannitol is commonly used as a pharmaceutical excipient for tablets; the most widely used oral dosage form for drug delivery. For tableting, mannitol is provided in two different forms: native crystals and textured particles. In order to optimize its formulation, a good understanding of the mechanical behavior mechanism of mannitol is necessary. Thus, the aim of this...
Source: International Journal of Pharmaceutics - June 2, 2018 Category: Drugs & Pharmacology Source Type: research

Comparative evaluation of powder flow parameters with reference to particle size and shape
This study showed that while the various flow characterisation techniques were different in terms of their applications, there were common physical attributes that governed the measurements. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - June 2, 2018 Category: Drugs & Pharmacology Source Type: research

Improved design and characterization of PLGA/PLA-coated Chitosan based micro-implants for controlled release of hydrophilic drugs
Publication date: 25 August 2018 Source:International Journal of Pharmaceutics, Volume 547, Issues 1–2 Author(s): Soumyarwit Manna, Anna M. Donnell, Necati Kaval, Marwan F. Al-Rjoub, James J. Augsburger, Rupak K. Banerjee Repetitive intravitreal injections of Methotrexate (MTX), a hydrophilic chemotherapeutic drug, are currently used to treat selected vitreoretinal (VR) diseases, such as intraocular lymphoma. To avoid complications associated with the rapid release of MTX from the injections, a Polylactic acid (PLA) and Chitosan (CS)-based MTX micro-implant prototype was fabricated in an earlier study, which showed ...
Source: International Journal of Pharmaceutics - June 2, 2018 Category: Drugs & Pharmacology Source Type: research

Development of ciprofloxacin-loaded poly(vinyl alcohol) dry powder formulations for lung delivery
This study aims to develop and characterize inhalable ciprofloxacin (CPx)-loaded poly(vinyl alcohol) (PVA) microparticles by a single-step spray-drying procedure. The optimization of the processing parameters was achieved by an orthogonal design of the most relevant processing parameters (polymer concentration, feed rate and inlet temperature). The obtained spray-dried particles showed a drug encapsulation efficiency higher than 90%. Furthermore, PVA-CPx formulations, with drug contents up to 10 wt%, showed a morphology and size suitable for inhalation, with a sustained release profile over 24 h. Data from Fourier tran...
Source: International Journal of Pharmaceutics - June 2, 2018 Category: Drugs & Pharmacology Source Type: research

Characterization of mannitol granules and powder: A comparative study using two flowability testers
Publication date: 25 August 2018 Source:International Journal of Pharmaceutics, Volume 547, Issues 1–2 Author(s): Yoshiko Takeuchi, Tomoka Tomita, Junko Kuroda, Akihiro Kageyu, Chihiro Yonekura, Yukiyoshi Hiramura, Kohei Tahara, Hirofumi Takeuchi In the manufacture of tablets, especially in direct tableting processes, the flowability of excipient powders and formulated powders is one of the most important characteristics. In the past two decades, orally disintegrating tablets (ODTs) have been prepared as popular solid dosage forms for elderly patients. Many types of mannitol granules have been developed and marketed...
Source: International Journal of Pharmaceutics - June 1, 2018 Category: Drugs & Pharmacology Source Type: research

In vitro and in vivo evaluation of an oral sustained release hepatoprotective caffeine loaded w/o Pickering emulsion formula – Containing wheat germ oil and stabilized by magnesium oxide nanoparticles
The objective of this study was to innovate an effective oral sustained release hepatoprotective formula for – the water soluble drug – caffeine. Caffeine is rapidly absorbed and eliminated which dictates frequent administration to achieve adequate therapeutic effect. A w/o Pickering emulsion incorporating caffeine in the internal phase was primed. It contained wheat germ oil and was stabilized by synthesized magnesium oxide nanoparticles (MgO NPs). Components selection was based on their antioxidant, hepatoprotective and anticarcinogenic effects. The MgO NPs were prepared via sol-gel method, and then were char...
Source: International Journal of Pharmaceutics - May 30, 2018 Category: Drugs & Pharmacology Source Type: research

Cyclodextrin-grafted poly(anhydride) nanoparticles for oral glibenclamide administration. In vivo evaluation using C. elegans
Publication date: 25 August 2018 Source:International Journal of Pharmaceutics, Volume 547, Issues 1–2 Author(s): David Lucio, María Cristina Martínez-Ohárriz, Zhongwei Gu, Yiyan He, Paula Aranaz, José Luis Vizmanos, Juan M. Irache The aim of this work was to prepare and evaluate cyclodextrins-modified poly(anhydride) nanoparticles to enhance the oral administration of glibenclamide. A conjugate polymer was synthesized by incorporating hydroxypropyl-β-cyclodextrin to the backbone of poly(methylvinyl ether-co-maleic anhydride) via Steglich reaction. The degree of substitution of anhyd...
Source: International Journal of Pharmaceutics - May 30, 2018 Category: Drugs & Pharmacology Source Type: research

A novel fusion protein attenuates collagen –induced arthritis by targeting interleukin 17A and tumor necrosis factor α
This study was undertaken to generate a novel dual targeting fusion protein (DTF), targeting tumor necrosis factor α (TNF-α) and interleukin 17A (IL-17A), and determine its anti-arthritis properties in vitro and in vivo. DTF consisted of an anti-IL-17A single chain variable fragment, a soluble TNF receptor 1, and an Fc fragment. Both clinical and histopathological evaluations suggest that DTF and etanercept can ameliorate collagen induced arthritis. However, the arthritis severity score of DTF-treated mice was lower than that of etanercept-treated mice. In addition, DTF was more potent than etanercept in decrea...
Source: International Journal of Pharmaceutics - May 30, 2018 Category: Drugs & Pharmacology Source Type: research

Comparison of high pressure homogenization and stirred bead milling for the production of nano-crystalline suspensions
Publication date: 25 August 2018 Source:International Journal of Pharmaceutics, Volume 547, Issues 1–2 Author(s): Mostafa Nakach, Jean-René Authelin, Marc-Antoine Perrin, Harivardhan Reddy Lakkireddy Currently, the two technologies primarily used for the manufacturing of nano-crystalline suspensions using top down process (i.e. wet milling) are high pressure homogenization (HPH) and stirred bead milling (SBM). These two technologies are based upon different mechanisms, i.e., cavitation forces for HPH and shear forces for stirred bead milling. In this article, the HPH and SBM technologies are compared in terms...
Source: International Journal of Pharmaceutics - May 28, 2018 Category: Drugs & Pharmacology Source Type: research

Enhanced cellular uptake and osteogenic differentiation efficiency of melatonin by inclusion complexation with 2-hydroxypropyl β-cyclodextrin
In this study, an inclusion complex of MLT with 2-hydroxypropyl β-cyclodextrin (HP-β-CD) was prepared to improve the water solubility, and the osteogenic differentiation ability of the inclusion complex was investigated in MC3T3-E1 cells. The formation of HP-β-CD/MLT inclusion complex was confirmed by 1H and 13C nuclear magnetic resonance spectroscopy and wide-angle X-ray diffraction. The water solubility of MLT increased linearly upon addition of HP-β-CD because of the formation of the inclusion complex. Additionally, treatment of the cells with HP-β-CD/MLT inclusion complex showed higher uptake a...
Source: International Journal of Pharmaceutics - May 27, 2018 Category: Drugs & Pharmacology Source Type: research

Combined effects of the drug distribution and mucus diffusion properties of self-microemulsifying drug delivery systems on the oral absorption of fenofibrate
We present the absorption improvement mechanism of fenofibrate (FFB), a Biopharmaceutics Classification System (BCS) class II drug, from self-microemulsifying drug delivery systems (SMEDDS), centered on improving the diffusion of FFB through the unstirred water layer (UWL). Four SMEDDS formulations containing Labrafac™ lipophile WL 1349 (WL1349) or Labrafil® M 1944CS (M1944) oils and NIKKOL HCO-40 (HCO40) or NIKKOL HCO-60 (HCO60) surfactants were prepared. Every SMEDDS formulation formed microemulsion droplets of approximately 30 nm. In vitro tests showed that the microemulsion droplets containing M1944 had rel...
Source: International Journal of Pharmaceutics - May 26, 2018 Category: Drugs & Pharmacology Source Type: research

Improved delivery of PLGA microparticles and microparticle-cell scaffolds in clinical needle gauges using modified viscosity formulations
Publication date: 30 July 2018 Source:International Journal of Pharmaceutics, Volume 546, Issues 1–2 Author(s): Omar Qutachi, Emma J. Wright, Gemma Bray, Omar A. Hamid, Felicity R.A.J. Rose, Kevin M. Shakesheff, Derfogail Delcassian Polymer microparticles are widely used as acellular drug delivery platforms in regenerative medicine, and have emerging potential as cellular scaffolds for therapeutic cell delivery. In the clinic, PLGA microparticles are typically administered intramuscularly or subcutaneously, with the clinician and clinical application site determining the precise needle gauge used for delivery. Here,...
Source: International Journal of Pharmaceutics - May 26, 2018 Category: Drugs & Pharmacology Source Type: research

The rheological and textural characterization of Soluplus ®/Vitamin E composites
In this study, Soluplus® was dissolved under heat in vitamin E at increasing concentrations from 0 to 40% (by weight). The flow behavior of the Soluplus®/Vitamin E composites was determined by applying shear stress using an advanced AR2000 rheometer. Under the linear viscoelastic region (LVR), the rheological properties of the blends such as dynamic viscosity (η′), storage modulus (G′), loss modulus (G″), and the phase angle tangent (tan δ) were measured. Hardness, adhesiveness, and cohesiveness of the blends were also measured with a TA.XT plus texture analyzer. Rheological analysis sho...
Source: International Journal of Pharmaceutics - May 26, 2018 Category: Drugs & Pharmacology Source Type: research

Model-based NIR spectroscopy implementation for in-line assay monitoring during a pharmaceutical suspension manufacturing process
Publication date: 30 July 2018 Source:International Journal of Pharmaceutics, Volume 546, Issues 1–2 Author(s): Maxim Verstraeten, Daan Van Hauwermeiren, Mario Hellings, Eline Hermans, Jeroen Geens, Chris Vervaet, Ingmar Nopens, Thomas De Beer The implementation of Process Analytical Technology (PAT) instruments is generally achieved stochastically. Sub-optimal PAT locations could introduce variation in the measurements which is not related to the analyte of interest. For this reason, rational approaches should be considered to establish an optimal sensor placement where relevant measurements are possible and the im...
Source: International Journal of Pharmaceutics - May 26, 2018 Category: Drugs & Pharmacology Source Type: research

The effect of the composition of a fixed dose combination on bioequivalence results
Publication date: 30 July 2018 Source:International Journal of Pharmaceutics, Volume 546, Issues 1–2 Author(s): Jana Šalandová, Aleš Franc, Jiří Hofmann, Aleksandra Dumicic, Lenka Kukačková, Tereza Červená, Josef Beránek, Jan Srbek, Andrej Repický, Beata Vladovičová, David Vetchý The purpose of this work was to develop a new supergeneric product Meloxicam/Omeprazole. Such a combination brings a benefit in terms of decreasing side effects for the patients using meloxicam. The new combination is composed of a meloxicam powder blend (MPB) and ome...
Source: International Journal of Pharmaceutics - May 26, 2018 Category: Drugs & Pharmacology Source Type: research

Effect of excipient properties, water activity, and water content on the disproportionation of a pharmaceutical salt
Publication date: 30 July 2018 Source:International Journal of Pharmaceutics, Volume 546, Issues 1–2 Author(s): Mitulkumar A. Patel, Suman Luthra, Sheri L. Shamblin, Kapildev K. Arora, Joseph F. Krzyzaniak, Lynne S. Taylor Excipients are crucial components of most pharmaceutical formulations. In the case of a solid oral dosage formulation containing the salt form of a weakly ionizable drug, excipient selection is critical, as some excipients are known to cause salt disproportionation (conversion of salt to the free form). Therefore, robust formulation design necessitates an in-depth understanding of the factors impa...
Source: International Journal of Pharmaceutics - May 26, 2018 Category: Drugs & Pharmacology Source Type: research